药物化学生物学。主要方向为抗肿瘤药物的设计、合成与生物学活性研究，化学生物学

1998-08--2001-08   复旦大学化学系与中国科学院上海有机化学研究所联合培养   生物有机化学博士
1995-09--1998-07   中国药科大学    药物化学硕士

1991年9月~ 1995年7月 化学制药本科，中国药科大学 

1995年9月~ 1998年7月 药物化学硕士，中国药科大学 
1998年9月~ 2001年7月 有机化学博士，复旦大学化学系（与中国科学院上海有机化学研究所联合培养）

  2001年12月~ 2005年2月 博士后研究，美国密西根大学肿瘤中心（the University of Michigan，Ann Arbor）
  2005年3月~ 2006年3月 Research Investigator, 美国密西根大学医学院

   

2023-05~现在, 中国科学院上海有机化学研究所, 研究员
2016-06~现在, 暨南大学, 暨南大学药学院院长（2016-2021），教授
2006-05~2016-06,中科院广州生物医药与健康研究院, 研究员
2005-03~2006-03,美国密西根大学医学院, Research Investigator
2001-12~2005-02,美国密西根大学肿瘤中心, 博士后研究

2023-04-30-今,The Innovation Medicine, Editorial Board Member,
2022-12-31-今,Science Bulletin Life Science, Editorial Board Member,
2022-12-31-今,China Science Life Science, Editorial Board Member,
2022-01-01-今,iScience, Advisory Editorial Board Member
2018-01-01-今,J.Med.Chem, Associate Editor
2015-07-01-今,中国药学会药物化学专业委员会, 副主委
2015-01-01-2017-12-31,MedChemComm, Associate Editor

2022, 吴阶平- 保罗 杨森医药科技奖（吴杨奖，Wu Jieping-Paul Janssen Medical & Pharmaceutical Awards）

2022，美国Prostate Cancer Foundation （PCF） TACTICAL Award

2022，中国药学会最美科技工作者

2018， 国家教学成果二等奖

2018，长江学者特聘教授

2017, 中国卫计委突出贡献中青年专家

2016, 科技创新创业领军人才

2016, Fellow, the Royal Society of Chemistry (UK, FRSC)

2015, 科技部人才推进计划

2014, 国家杰出青年基金获得者

2014, 广东省南粤百杰

2012, 国务院政府津贴

2012, 无锡药明康德生命化学奖

2009，第十届丁颖科技奖

2008，中科院%%%%

针对肿瘤临床耐药等重大需求，成功设计合成了：

1）中国首个克服Bcr-Abl^T315I突变耐药的抗白血病新药Olverembatinib（耐立克Ò，2021年获批上市），被美国FDA和欧洲委员会授予“孤儿药”资格；

2）克服非小细胞肺癌耐药的候选药物ASK120067（已提交新药上市申请（NDA））；

3）高效的Axl抑制剂HH30134（中、澳临床研究，www.clinicaltrials.gov, NCT 04746612）

4）世界首个选择性ZAK抑制剂、DDR1抑制剂、Akt3降解剂等类药性先导化合物。

（一）GDZ824（HQP1351）系列专利（2021年获批上市，奥雷巴替尼）。

(1)    杂环炔苯类化合物及其药用组合物和应用。中国发明专利。专利号：ZL201010216603.7授权时间：2013-7-24。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。申请人：中国科学院广州生物医药与健康研究，

进入以下外国国家阶段：

(2)    HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。美国发明专利。专利号：US8846671，授权时间2014-09-30。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

(3)    HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。日本发明专利。专利号：JP5756518，授权时间2015-06-05。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

(4)    HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。澳大利亚发明专利。专利号：AU20110274192，授权时间2015-02-19。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

 (5)  HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。韩国发明专利。专利号：KR10-1570456，授权时间2015-11-13。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

(6)    HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。加拿大发明专利。专利号：CA2804347，授权时间2016-07-05。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

(7)    HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。以色列发明专利。专利号：IL223983，授权时间2018-06-28。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

(8)    HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。再进入中国发明专利，专利号： ZL 201180040373.6，授权时间2014-12-10。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

 (9)吡唑并吡啶炔苯类化合物及其药用组合物和应用，中国发明专利，专利号ZL 201210018905.2， 授权日：2015-12-16。*丁克、冯玉冰、陆小云、潘小芬、张章、龙活尤、任小梅、李伟华

(10) HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF。欧洲发明专利。申请号：EP11800049.6，申请时间2013-12-20。丁克，王德平，裴端卿，张章，沈梦婕，罗坤，冯玉冰。

（二）120067（ASK120067，已提交新药上市申请 （NDA））系列专利。

(1)       2-氨基嘧啶类化合物及其药物组合物和应用。中国发明专利，CN201410682756.9。申请日：2014-11-24，PCT申请：PCT/CN2015/094954 2015-11-18。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

申请人：中科院上海药物化学所，中国科学院广州生物医药与健康研究，江苏奥赛康药业有限公司

进入以下外国国家阶段：

(2)      2-氨基嘧啶类化合物及其药物组合物和应用（美国）。美国发明专利，  15/529,333。2017-5-24。专利号：US10059694，授权日：2018-08-28。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(3)     2-氨基嘧啶类化合物及其药物组合物和应用（日本）。日本发明专利，申请号：2017-528838。2017-5-24。专利号：JP6474068，授权日：2019-02-08。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(4)     2-氨基嘧啶类化合物及其药物组合物和应用（澳大利亚）。澳大利亚发明专利，申请号：2015353210。2017-6-20。专利号：AU2015353210，授权日：2019-08-15。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(5)     2-氨基嘧啶类化合物及其药物组合物和应用（韩国）。韩国发明专利，申请号：10-2017-7017442。2017-6-23。专利号：KR10-1941929，授权日：2019-01-18。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(6)     2-氨基嘧啶类化合物及其药物组合物和应用（新西兰）。新西兰发明专利，专利号：NZ733009。授权日：2019-01-29。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(7)     2-氨基嘧啶类化合物及其药物组合物和应用（新加坡）。新加坡发明专利，申请号：SG11201704244S。申请日：2017-05-24。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(8)     2-氨基嘧啶类化合物及其药物组合物和应用（俄罗斯）。俄罗斯发明专利，申请号：RU2017122062。2017-05-23。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕.

(9)     2-氨基嘧啶类化合物及其药物组合物和应用（欧洲）。欧洲发明专利，申请号：EP15863532.6。申请日：2017-06-20。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(10)  2-氨基嘧啶类化合物及其药物组合物和应用（以色列）。以色列发明专利，申请号：IL252477。申请日：2017-05-24。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(11)  2-氨基嘧啶类化合物及其药物组合物和应用（加拿大）。加拿大发明专利，申请号：CA2968633。申请日：2017-05-23。丁克，丁健，陈成斌，耿美玉，任小梅，谢华，涂正超，陈奕。

(12)  一种2-氨基嘧啶类化合物的多晶型形式。中国发明专利，申请号：CN201710368894.3，申请日：2017-05-23。梅雪锋，丁克，丁健，谢华，陈成斌，赵俊，宋婷婷，宗在伟，孙敏。

(13)  一种2-氨基嘧啶类化合物的多晶型形式。PCT号：PCT/CN2017/085566，申请日：2017-05-23。 梅雪锋，丁克，丁健，谢华，陈成斌。

（三）JND30134化合物专利（中澳临床研究）。

1.        发明名称:取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用       专利类型：中国发明专利，专利号：ZL201510509618.5，申请日：2015-8-18 授权日2019-4-5，发明人：丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。申请人：暨南大学  中国科学院上海药物研究所。 PCT申请PCT/CN2016/095813  国际申请日：2016年8月18日

2.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。日本专利号：JP6530857，授权日：2019年5月24日。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

3.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。澳大利亚专利申请已于2018年2月14日成功提交，澳大利亚专利号为AU2016309833，授权日：2019年9月5日。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

4.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。欧洲专利申请已于2018年2月14日成功提交，欧洲申请号为EP16836661.5。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

5.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。美国专利申请已于2018年2月15日成功提交，美国申请号为：US15/752,896。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

6.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。以色列专利申请已于2018年2月12日成功提交，申请号为IL257481。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

7.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。韩国专利申请已于2018年3月16日成功提交，韩国申请号为KR2018-7007648。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

8.        取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用。再次进入中国专利，再进入中国阶段2018年4月4日，申请号为：CN201680058335.6。丁克，耿美玉，谈理，丁健，张章，艾菁，任小梅，高冬林，涂正超，陆小云，张冬梅。

9.        喹啉或喹唑啉类化合物及其应用，申请号：201810277244.2，申请日：2018年3月30日， PCT申请号：PCT/CN2019/080659，2019/3/29国际申请日。暨南大学; 中国科学院上海药物研究所。发明人：丁克，耿美玉，陈成斌，丁健，谈理，艾菁，张章，彭霞，任小梅，季寅淳 ，涂正超，戴阳 ，陆小云。

10.     3-氨基吡唑类化合物及其应用，申请号：201810260759.1，申请日：2018年3月27日， PCT申请号：PCT/CN2019/079733，2019/3/26国际申请日。暨南大学; 中国科学院上海药物研究所。发明人：丁克，耿美玉，陈成斌，丁健，谈理，艾菁，张章，彭霞，任小梅，季寅淳 ，段云鑫，戴阳，涂正超，陆小云。

二、其他已授权专利

• 1.        2－吡啶－b酮类化合物的应用.。

• 专利类型：中国发明专利，专利号：ZL 200810219057.5授权时间: 2011.04.27  IPC分类号：C07B43/04

• 发 明 人：*丁克、王德平

2.        化合物ABT-263的合成方法.

专利类型：中国发明专利，专利号：ZL 200810025940.0授权时间: 2011.04.27  IPC分类号：C07D295/14

发 明 人：*丁克、王广军、张虎山、周净

3.        吡啶基噻唑胺类化合物及其应用.

专利类型：中国发明专利，专利号：ZL 200910193571.0。授权时间:2011.12.26 IPC分类号：C07D417/14

发 明 人：*丁克、王德平、裴端卿、潘景轩、张章、冯玉冰、罗坤、甘继荣、庄晓曦、段磊

4.        用作雌激素相关受体调节剂的化合物及其应用。

专利类型：中国发明专利，专利号：ZL 200810026782.0。授权时间：2011.12.28 IPC分类号：C07D471/04

发 明 人：*丁克、黄志伟、康战方、周曦、彭丽洁

5.        一种吡唑类化合物及其组合物和应用.

专利类型：中国发明专利，专利号：ZL 201019050010.5. 授权时间:2012.03.21 IPC分类号：C07D231/12

发 明 人：*丁克、刘秀洁、王东业、惠晓艳、徐爱民、吴东海.

6.        二芳基脲类化合物及其在抗肿瘤药物制备中的应用

专利类型：中国发明专利，专利号：ZL 200810029024.4。授权时间:2012.03.21 IPC分类号：C07D295/14

发 明 人：*丁克、裴端卿、王德平、段磊、任小梅、周净、甘继荣、周凤涛、张章

7.        一种吲哚衍生物的合成方法.

专利类型： 中国发明专利，专利号ZL200910214457.1授权时间:2012.06.06  IPC分类号：C07D495/14

发 明 人：*丁克、李正球、蔡倩

8.        雌激素相关受体调节剂及其应用。

专利类型：中国发明专利，专利号ZL 200810029586.9。授权时间:2013.1.23

IPC分类号：C07D471/04

发 明 人：*丁克、黄志伟、彭丽洁

9.        用作蛋白聚糖酶调节剂的化合物及其应用。

专利类型：中国发明专利，专利号：ZL201110143591.4授权时间:2014.06.25 IPC分类号：C07D295/14

发 明 人：*丁克、彭丽洁、段磊

10.     The compounds as the estrogen related receptors modulators and the uses  thereof

专利类型：日本发明专利，专利号：JP5524091授权时间2014.4.18 IPC分类号：C07D471/04

发 明 人：*丁克、黄志伟、康战方、周曦、彭丽洁

11.     The compounds as the estrogen related receptors modulators and the uses  thereof

专利类型：澳大利亚发明专利，专利号：AU2009225171授权时间2014.11.20 IPC分类号：C07D471/04

发 明 人：*丁克、黄志伟、康战方、周曦、彭丽洁

12.     Compounds as the estrogen related receptors modulators and the uses  thereof

专利类型：美国发明专利，专利号：US8853221授权时间：2014.10.7 IPC分类号：C07D471/04

发 明 人：*丁克、黄志伟、康战方、周曦、彭丽洁

13.     Compounds as the estrogen related receptors modulators and the uses  thereof

专利类型：澳大利亚发明专利，专利号：2009270363授权时间2014.6.26 IPC分类号：C07D471/04

发 明 人：*丁克、黄志伟、康战方、周曦、彭丽洁

14.     吉非替尼的制备方法

专利类型：中国发明专利，专利号 201210265997. 4。授权时间：2015.8.5

 IPC分类号：C07D239/94

发 明 人：*丁克、李伟华、陆小云、李宇鹏、 沈梦婕

15.     Ponatinib的制备方法

专利类型：中国发明专利，专利号 201210265384.0。授权时间：2015.12.16 IPC分类号：C07D487/04

发 明 人：*丁克、冯玉冰、陆小云、李伟华、李宇鹏、 沈梦婕

16.     7-氧代吡啶并嘧啶类化合物及其药用组合物和应用

专利类型：中国发明专利，专利号：201210480885.0授权时间：2015.6.17 IPC分类号：C07D471/04

发 明 人：*丁克、徐田锋、丁芳

17.     嘧啶并嘧啶酮类化合物及其药用组合物及其应用

专利类型：中国发明专利，专利号：201110156399.9授权时间：2016.3.9 IPC分类号：C07D487/04

发 明 人：*丁克、常少华、徐石林、张连文、涂正超、丁健、耿美玉、陈奕。

18.     嘧啶并三环或嘧啶并四环类化合物及其药用组合物和应用

专利类型：中国发明专利，专利号 201210266329.3  2012.7.30 授权日：2016-5-18

发 明 人：*丁克、徐田锋、常少华、张连文、罗金凤、徐石林、肖宜平、涂正超

19.     发明名称：嘧啶并杂环类化合物及其药用组合物和应用

专利类型：中国发明专利，专利号 201310365460.X 2013-8-20授权日：2016-9-7

发明人：丁克 徐石林 徐田锋  张连文 丁芳 涂正超  陆小云 丁健 耿美玉

20.     5-噻唑酰胺类化合物及其生物学应用.

专利类型：中国发明专利，专利号201010265115.5 申请日期2010.8.27 授权日期2016/8/3

发 明 人：朱孝峰 *丁克、邓蓉、常少华.

21.     杂环苯甲酰胺类化合物、药用组合物及其应用

专利类型：中国发明专利，专利号 201210236713. 9。2012-7-10 授权2016/8/17

发 明 人：*丁克、李宇鹏、沈梦婕、龙活尤、张章、冷芳、陆小云

22.     用于盘状结构域受体小分子抑制剂的化合物及其应用

专利类型：中国发明专利，专利号 201310042505.X 2013-2-1授权2016/9/28

发 明 人：*丁克、高明山、冯玉冰，李伟华

23.     用于用作雌激素相关受体调节剂的化合物及其应用

专利类型：中国发明专利，专利号201310157230.4  2013-5-20授权2016/6/29

发 明 人：*丁克，徐石林，庄晓曦; 潘小芬，张章，段磊，陆小云

24.     发明名称：5-芳基酚-2-烷基取代并咪唑类化合物和应用

专利类型：中国发明专利，专利号 201410069823.X 2014-2-27 授权日：2018-4-27

发明人：丁克 程辉敏 李迎君 谈理 王雪聪 张章 庄晓曦 龙活尤

25.     发明名称：埃罗替尼的制备方法

专利类型：中国发明专利，专利号 201410127452.6 2014-3-31 授权日：2017-10-17

发明人：丁克 陆小云 李伟华

26.     发明名称：吡唑并[1,5-a]吡啶类化合物及其药用组合物和应用   

专利类型：中国发明专利，专利号：CN201510460751.6  2015-7-31 授权日：2018-3-27及PCT提交  PCT/CN2015/086852  2015-8-13

发明人：陆小云，汤健，丁克，张天宇，涂正超，伍甜，万军庭，曹元元 IPC分类号 :C07D471/04

美国专利号：US 10,155,756授权日：2018年12月18日

专利期限：从2015年8月13日至2035年8月13日

27.     发明名称：磺酰胺基芳基炔类化合物及其用途     

专利类型：中国发明专利，专利号：201410753013.6    2014-12-9 授权日：2018-6-12

发明人：丁克，李迎君，程辉敏，任小梅，张章，庄晓曦，龙活尤，涂正超

28.     嘧啶并二氮杂卓类化合物及其药用组合物和应用

专利类型：中国发明专利，专利号 201210109797.X。2015.11.11日授权

发 明 人：*丁克、徐石林、常少华、张连文、涂正超

29.     发明名称：N-4-三氟甲基苯基水杨酰胺衍生物的制备方法和应用

专利类型：中国发明专利，专利号 201410073672.5 2014-2-28  授权日：2019.6.4

发明人：丁克 陆小云  张天宇 汤健 鲁明辉 李宇鹏 张章 梁镇兴 钱政江

30.     炔苯基苯磺酰胺类选择性ZAK抑制剂及其应用 2016110825090  2016/11/30  专利号： 201611082509.0. 授权日：2019-8-16 暨南大学 丁克，陆小云，常玉，涂正超; 黄志扬，张庆文，罗金凤，张章，徐布Shibu. M. A.

 

三、其他在申请专利：12件

1.        嘧啶并吡啶酮或者吡啶并吡啶酮类化合物及其应用 2017105916446  2017/7/19 暨南大学; 中国科学院上海药物研究所; 江苏奥赛康药业股份有限公司 发明人：丁克，丁健，申佳奕，耿美玉，陆小云，谢华，孙敏，宗在伟

2.        2-氨基嘧啶类化合物及其应用 暨南大学 2017101134878  2017/2/28 发明人：丁克 ，陆小云，莫程，李学强，任小梅，张章; 涂正超，罗金凤，杰弗里.布鲁斯.斯美而; 亚当.逢.帕特森(Adam Vorn Patterson)

3.        四氮唑类分子探针化合物或组合物及其应用 2017109407892  2017/9/30 暨南大学 发明人：丁克， 李正球，程柯

4.        Adam Vorn PATTERSON, Jeffrey Bruce SMAILL, ASHOORZADEH, Amir, Christopher Paul GUISE, Christopher John SQUIRE, Xueqiang LI, Ke DING, Xiaomei REN, Shuang JIANG, Zhengchao TU. FGFR KINASE INHIBITORS AND PHARMACEUTICAL USES, 新西兰发明专利NZ729651。2017-3-3

5.        嘧啶并嘧啶酮类化合物及其药用组合物和应用，201711258448.3， 2017/11/29，暨南大学; 中国科学院上海药物研究所，丁克，寻秋菊，丁健，陆小云，谢华，张章，耿美玉，任小梅，童林江。   

6.        2-氨基嘧啶类化合物及其应用，申请号：201810230760.X，申请日：2018年3月20日，暨南大学; 中国科学院上海药物研究所。发明人：丁克，丁健，李姗，谢华，陆小云，耿美玉，任小梅，童林江。

7.        靶向泛素化降解ERRα蛋白的化合物及其药用组合物和应用，申请号：201811445971.1，申请日：2018年11月29日，暨南大学; 发明人：丁克，彭丽洁，张振声，任小梅，张章，雷冲，李姗。

8.        GZD824及其药学上可接受的盐在治疗疾病中的新应用，申请号：201811184991.8，申请日：2018年10月11日，暨南大学; 发明人：丁克，张章，王雨婷。

9.        2-氨基嘧啶类化合物及其应用，申请号：201811517594.8，申请日：2018年12月12日，暨南大学; 中国科学院上海药物研究所。发明人：丁克，丁健，陆小云，耿美玉，李姗，谢华，陈灏，童林江， 任小梅，冯芳。

10.     丙烯酰胺类化合物及其应用 申请号：201910044871.6，申请日：2019年1月17日，暨南大学 发明人：丁克， 李正球，国翠平，王鑫，徐嘉乾，胡俊，肖湘成

11.     杂环苯磺酰胺类化合物及其应用申请号：201910001981.4 ，申请日：2019年1月2日，暨南大学;发明人：丁克，陆小云，阳建章，黄志杨，徐布，涂正超。

12.     氮杂环丙烯类化合物及其制备方法和应用，申 请 号：2019102950853 

申 请 日：2019年04月12日，申请人：暨南大学；发明人：李正球，麻楠，叶文才，丁克，胡俊

13.     2-吲哚酮类ERRα反向激动剂及其药物组合物和应用，申请号：CN201910894236.7，申 请 日：2019年9月21日，申请人：暨南大学；发明人：丁克，李姗，彭丽洁，司鸿飞，张章，任小梅，雷冲

2023

1）        Guan, T.; Li, M.; Song, Y.; Chen, J.; Tang, J.; Zhang, C.; Wen, Y.; Yang, X.; Huang, L.; Zhu, Y.; Wang, H.; Ding, K.* Zheng, J.* Zhang, H.*; Liu, T.* Phosphorylation of USP29 by CDK1 Governs TWIST1 Stability and Oncogenic Functions. Adv. Sci. 2023 https://doi.org/10.1002/advs.202205873

2）        Lv, S.; Xu, F.; Fan, Y.; Ding, K.* & Li, Z.* Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J. Med. Chem. 2023, https://doi.org/10.1021/acs.jmedchem.2c01889

3）       He, R.; Song, Z.; Bai, Y.; He, S.; Huang, J.; Wang, Y.; Zhou, F.; Huang, W.; Guo, J.; Wan, Z.; Tu, Z.-C.; Re, X.; Zhang, Z.; Xu, J.; & Ding, K.* Discovery of AXL Degraders with Improved Potencies in Triple-Negative Breast Cancer (TNBC) Cells. J. Med. Chem. 2023, 66(3), 1873–1891.

4）       Lai, M.; Zhang, T.; Chen, H.; Song, P.; Tong, L.; Chen, J.; Liu, Y.; Ning, Y.; Feng, F.; Li, Y.; Tang, H.; Chen, Y.; Fang, Y.; Lu, X.; Geng, M.; Ding, K.; * Yu, K.*; Ding, J.*; Xie, H.* Discovery of HCD3514 as a potent EGFR inhibitor against C797S mutation in vitro and in vivo. J. Cancer, 2023, 14(1), 152.

2022

1)           Zhang, Y.; Chan, S.; He, R.; Liu, Y.; Song, X.; Tu, Z.-Z.; Ren, X.; Zhou, Y.; Zhang, Z.*; Wang, Z.*; Zhou, F.*; Ding. K.* 1-Methyl-3-((4-(quinolin-4-yloxy)phenyl) amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during Transfection (RET) kinase inhibitors capable of suppressing resistant mutants in solvent-front regions. Eur. J. Med. Chem. 2022, 244, 114862

2)           Wang, Y.; Zhou, Y.; Shi, C.; Liu, J.; Lv, G.; Huang, H, Li, S.; Duan, L.; Zheng, X.; Liu, Y.; Zhou, H.; Wang, Y.; Ding, K.*; Sun, P.*; Huang, Y.*; Lu, X.*; Zhang, Z.-M.* A toxin-deformation dependent inhibition mechanism in the T7SS toxin-antitoxin system of Gram-positive bacteria. Nature Commu. 2022, 13, 6434.

3)           Wang, J.; Zhou, Y.; Tang, X.; Yu, X.; Wang, Y.; Chan, S.; Song, X.; Tu, Z.-C.; Zhang, Z.-M.; Lu, X.*; Zhang, Z.*; Ding, K.* JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo. Molecules 2022, 27, 6500.

4)           Shu, S.; Liu, H.; Yang, J.; Tang, H.; Li, H.; Liu, Z.; Zhou, M.; Zhu, F.; Hu, Z.; Ding, K.; Lu, X.; Nie, J.* Targeted inhibition of ZAK ameliorates renal interstitial fibrosis. 2022, 246, 49 – 65. DOI: 10.1016/j.trsl.2022.03.002

5)           Chen, Z.; Ke, R.; Song, Z.; Zhou, Y.; Ren, X.; Huang, W.; Wang, Z.*, Ding, K.* A novel photocaged B-RafV600E inhibitor toward precise melanoma treatment. Bioorg. Med. Chem. Lett. 2022, 64, 128683

6)           Shen, C.; Zhang, D.; Xu, F.; Yang, Y.; Tan, Y.; Zhang, Q.*; Li, L.; Ding, K.; Li, Z.* Two-photon fluorescent turn-on probes for highly efficient detection and profiling of thiols in live cells and tissues. Biol. Chem. 2022 403, 445 – 451.

7)            Lyu, P.; Jiang, K.; Zhou, Y.; Hu, J.; Chang, Y.; Zhang, Z.; Hunag, M, Zhang, Z.-M.; Ding, K.*; Hao, P.; *, Lin, L.*; Li, Z.* Proteome-wide Identification of Off-Targets of a Potent EGFRL858R/T790MMutant Inhibitor. ACS Med. Chem. Lett. 2022, 13, 292-297.

8)           Liu, Y.; Lai, M.; Li, S.; Wang, Y.; Feng, F.; Zhang, T.; Tong, L.; Zhang, M.; Cheng, H.; Chen, Y.; Song, P.; Li, Y.; Bai, G.；Ning, Y.； Tang，H.; Fang, Y.; Chen, Y.; Lu, X.; Geng, M.; Ding, K*; Yu, K.*; Xie, H.*; Ding, J.* LS-106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo. Cancer Science, 2022, 113, 709-720.

9)           Si. H.; Wang, J.; He, R.; Yu, X.; Li, S.; Huang, J.; Li, J.; Tang, X.; Song, X.; Tu, Z.-C.; Zhang, Z.*, Ding, K.* Identification of U937JAK3-M511I Acute Myeloid Leukemia Cells as a Sensitive Model to JAK3 Inhibitor. Frontiers in Oncology 2022, 11, 807200.

10)        Chan, S.; Zhang, Y.; Wang, J.; Yu, Q.; Peng, X.; Zou, J.; Zhou, L.; Tan, L.; Duan, Y.; Zhou, Y.; Hur, H.; Ai, J.*; Wang, Z.*; Ren, X.*; Zhang, Z.*; Ding, K*. Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors. J. Med. Chem. 2022, 65, 22, 15374–15390.

11)        Xu, F.; Zhang, X.; Chen, Z.; He, S.; Guo, J.; Yu, L.; Wang, Y.; Hou, C.; AI-furas, H.; Zheng, Z.; Smaill, J. B.; Patterson, A. V.; Zhang, Z.-M.; Chen, L.*; Ren, X.*; and Ding, K.* Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells. J. Med. Chem. 2022, 65, 20, 14032–14048.

12)        Yang, J.; Chang, Y.; Tien, J. C.-Y.; Wang, Z.; Zhou, Y.; Zhang, P.; Huang, W.; Vo, J.; Apel, I. J.; Wang, C.; Zeng, V. Z.; Cheng, Y.; Li, S.; Wang, G. X.*; Chinnaiyan, A. M.*; and Ding, K.* Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13. J. Med. Chem. 2022, 65, 16, 11066–11083

13)        Li, S.; Zhang, P.; Xu, F.; Hu, S.; Liu, J.; Tan, Y.; Tu, Z.; Sun, H.; Zhang, Z.-M.; He, Q.-Y.; Sun, P.*; Ding, K.*; and Li, Z.* Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J. Med. Chem. 2022, 65, 15, 10408–10418.

14)        Li, S.; Si, H.; Song, X.; Lei, C.; He, X.; Wang, J.; Liu, Y.; Zhou, Y.; Song,J.-G.; Peng, L.; Tang, X.; Chan, S.; Ren, X.; Tu, Z.-C.; Li*, Z.*; Wang*, Z.&； Zhang, Z.*; and Ding, K.* Discovery of Hexahydrofuro[3,2-b]furans as New Kinase-Selective and Orally Bioavailable JAK3 Inhibitors for the Treatment of Leukemia Harboring a JAK3 Activating Mutant. J. Med. Chem. 2022, 65, 15, 10674–10690.

15)        Chen, H.; Lai, M.; Zhang, T.; Chen, Y.; Tong, L.; Zhu, S.; Zhou, Y.; Ren, X.; Ding, J.; Xie, H.*; Lu, X.*; and Ding, K.* Conformational Constrained 4-(1-Sulfonyl-3-indol)yl -2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations. J. Med. Chem. 2022, 65, 9, 6840–6858.

16)        Wang, Z.; Wang, J.; Wang, Y.; Xiang, S.; Song, X.; Tu, Z.-C.; Zhou, Y.; Zhang, Z.-M.*; Zhang, Z.*, Ding, K.*; and Lu, X.* Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance. J. Med. Chem. 2022, 65, 8, 6325–6337.

17)        Zhang, Z.; Li, J.; Chen, H.; Huang, J.; Song, X.; Tu, Z.-C.; Zhang, Z.; Peng, L.*; Zhou, Y.*; and Ding, K.* Design, Synthesis, and Biological Evaluation of 2-Formyl Tetrahydronaphthyridine Urea Derivatives as New Selective Covalently Reversible FGFR4 Inhibitors. J. Med. Chem. 2022, 65, 4, 3249–3265.

18)        Mao, L.; Peng, L.; Ren, X.; Chu, Y.; Lin, W.; Nie, T.; Lin, W.; Libby, A.; Xu, Y.; Chang, Y.; Lei, C.; Lommes, K.; Liu, J.; Levi, M.; Wu, D.; Hui, X*; and Ding, K.* Discovery of JND003 as a New Selective Estrogen-Related Receptor α Agonist Alleviating Nonalcoholic Fatty Liver Disease and Insulin Resistance. ACS Bio. Med. Chem. Au 2022, 2, 3, 282–296.

19)        Lu, J.; Huang, Y.; Huang, J.; He, R.; Huang, M.; Lu, X.; Xu, Y.; Zhou, F.*; Zhang, Z.* and Ding, K.* Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders. J. Med. Chem. 2022, 65, 3, 2313–2328.

20)        Wang, Z.*; Huang, W.; Zhou, K.; Ren, X.; and Ding, K.* Targeting the Non-Catalytic Functions: a New Paradigm for Kinase Drug Discovery? J. Med. Chem. 2022, 65, 3, 1735–1748.

21)        Li, S.; Zhang, T.; Zhu, S.-J.; Lei, C.; Lai, M.; Peng, L.; Tong, L.; Pang, Z.; Lu, X.; ding, J.; Ren, X.*; Yun, C.-H.*; Xie, H.*; and Ding, K.* Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFRT790M/C797S Mutants. ACS Med. Chem. Lett. 2022, 13, 2, 196–202.

2021

1)       Zhang, Z.; Wang, YJ.; Chen, XJ.; Song, XJ.; Tu, ZC.; Chen, YH.; Zhang, ZM.; Ding, K.* Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design. Bioorgan. Med. Chem. 2021, 50, 116457,  https://doi.org/10.1016/j.bmc.2021.116457

2)       Jin, YL.; Ding, K.; Li, HL.; Xue, MZ.; Shi, XK.; Wang, CY .; Pan, JX. Ponatinib efficiently kills imatinib-resistant chronic eosinophilic leukemia cells harboring gatekeeper mutant T674I FIP1L1-PDGFR alpha: roles of Mcl-1 and beta-catenin. Mol. Cancer. 2021, 20(1): 137, https://dx.doi.org/10.1186%2F1476-4598-13-17

3)       Xia, Y.; Zou, R.; Escouboue, M.; Zhong, L.; Zhu, CJ.; Pouzet, C.; Wu, XQ.; Wang, YJ .; Lv, G.; Zhou, HB.; Sun, PH.*; Ding, K.*; Deslandes, L.*; Yuan, SG.*; Zhang, ZM.* Secondary-structure switch regulates the substrate binding of a YopJ family acetyltransferase. Nat. Commun. 2021, 12, 5969, https://dx.doi.org/10.1038%2Fs41467-021-26183-1

4)       Fan, YL.; Si, HF.; Zhang, Z.; Zhong, L.; Sun, HY.; Zhu, CJ.; Yin, ZB.; Li, HL.; Tang, GH.; Yao, SQ.; Sun, PH.*; Zhang, ZM.*;  Ding, K.*; Li, ZQ.* J. Med. Chem. 2021, 64, 21, 15582-15592, https://doi.org/10.1021/acs.jmedchem.0c02024

5)       Shen, CZ.; Zhang, DT.; Xu, F.; Yang, Y.; Tan, Y.; Zhao, Q.; Li, L.; Ding, K.*; Li, ZQ.* Two-photon fluorescent turn-on probes for highly efficient detection and profiling of thiols in live cells and tissues. Biol. Chem. 2021,  10.1515/hsz-2021-0189

6)       Liu, Y.; Lv, S.; Peng, L.; Xie, C.; Gao, L.; Sun, H.; Lin, L.; Ding, K.*; Li, Z.*  Development and application of novel electrophilic warheads in target identification and drug discovery. Biochemical Pharmacology 2021, 190, 114636, https://doi.org/10.1016/j.bcp.2021.114636

7)       Jiang, K., Tang, X., Guo, J., He, R., Chan, S., Song, X., Tu, Z., Wang, Y., Ren, X., Ding, K.*, Zhang, Z.* GZD824 overcomes FGFR1-V561F/M mutant resistance in vitro and in vivo. Cancer medicine. 2021, 10(14), 4874–4884. https://doi.org/10.1002/cam4.4041

8)       Dai W., Liu S., Wang S., Zhao L., Yang X., Zhou J., Wang Y., Zhang J., Zhang P., Ding K., Li Y., Pan J.*. Activation of transmembrane receptor tyrosine kinase DDR1-STAT3 cascade by extracellular matrix remodeling promotes liver metastatic colonization in uveal melanoma. Signal Transduct Target Ther. 2021, 6(1), 176, https://dx.doi.org/10.1038%2Fs41392-021-00563-x

9)       Jiang, L., Wang, Y., Li, Q., Tu, Z., Zhu, S., Tu, S., Zhang, Z.*, Ding, K*, Lu, X.*  Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation. Acta pharmaceutica Sinica. B. 2021, 11(5), 1315–1328,  https://doi.org/10.1016/j.apsb.2020.11.009

10)    Deng, W.; Chen, X.; Jiang, K.; Song, X.; Huang, M.; Tu, Z.-C.; Zhang, Z.; Lin, X.; Ortega, R.; Patterson, A. V.; Smaill, J. B.; Ding, K.; Chen, S.*, Chen, Y.*, Lu, X.* Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors. ACS Med. Chem. Lett. 2021, 12, 647–652, https://doi.org/10.1021/acsmedchemlett.1c00052

11)    Huang, M.; Huang, Y.; Guo, J.; Yu, L.; Chang, Y.; Wang, X.; Luo, J.; Huang, Y.; Tu, Z.; Lu, X.; Xu, Y.; Zhang, ZM.*; Zhang, Z.*; Ding, K.* Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors. Eur. J. Med. Chem. 2021, 211, 113023. https://doi.org/10.1016/j.ejmech.2020.113023

12)    Qiao, Y.; Tien, J. E. C.; Simko, S. A.; Rajendiran, T.; Vo, J. N; Delekta, A. D.; Wang, L.; Xiao, L.; Hodge, N. B.; Desai, P.; Mendoza, S.; Juckette, K.; Xu, A.; Soni, T.; Su, F.; Wang, R.; Cao, X.; Yu, J.; Kryczek, I.; Wang, X.-M.; Wang, X.; Siddiqui, J.; Wang, Z.; Bernard, A.; Fernandez-Salas, E.; Navone, N. M.; Ellison, S. J.; Ding, K.; Eskelinen, E.-L.; Klionsky, D. J.; Zou, W.; Chinnaiyan, A. M. Autophagy inhibition by targeting PIKfyve potentiates response to immune checkpoint blockade in prostate cancer. Nature Cancer 2021, 2, 978–993

 

2020

1)       Fan, Z.; Tian, Y.; Chen, Z.; Liu, L.; Zhou, Q.; He, J.; Coleman, J.; Dong, C.; Li, N.; Huang, J.; Xu, C.; Zhang, Z.; Gao, S.; Zhou, P.*; Ding, K.*; & Chen, L.* Blocking interaction between SHP2 and PD‐1 denotes a novel opportunity for developing PD‐1 inhibitors. EMBO Mol. Med. 2020, e11571, https://doi.org/10.15252/emmm.201911571

2)         Zhang, X.; Xu, F.; Tong, L.; Zhang, T.; Xie, H.; Lu, X.; Ren, X.*; Ding, K.* Design and synthesis of selective degraders of EGFRL858R/T790M mutant. Eur. J. Med. Chem. 2020, https://doi.org/10.1016/j.ejmech.2020.112199.

3)         Zhang, T.; Qu, R.; Chan, S.; Lai, M; Tong, L.; Feng, F.; Chen, H.; Song, T.; Song, P.; Bai, G.; Liu, Y.; Wang, Y.; Li, Y.; Su, Y.; Shen, Y.; Sun, Y.; Chen, Y.; Geng, M.; Ding, K.*; Ding, J.* and Xie, H.* Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol. Cancer 2020, https://doi.org/10.1186/s12943-020-01202-9.

4)         Ma, N.; Hu, J.; Zhang, Z.-M.; Liu, W.; Huang, M.; Fan, Y.; Yin, X.; Wang, J.*; Ding, K.*; Ye, W* and Li. Z.* 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J. Am. Chem. Soc. 2020, https://doi.org/10.1021/jacs.9b12116

5)         Guo, J.; Zhang, Z.; Ding, K.* A patent review of discoidin domain receptor 1 (DDR1) modulators (2014-present). Expert Opinion on Therapeutic Patents 2020, https://doi.org/10.1080/13543776.2020.1732925

6)         Jiang, L.; Wang, X.; Wang, Y.; Xu, F.; Zhang, Z.*; Ding, K.*; Lu, X.* The synthesis and biological evaluation of sanguinarine derivatives as anti-non-small cell lung cancer agents. RSC Med. Chem. 2020, 11, 293-296

7)         Xu, J.; Zhang, Z.; Lin, L.; Sun, H.; White, L. V.; Ding, K.*; Li, Z.*Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor. ACS Med. Chem. Lett. 2020, https://doi.org/10.1021/acsmedchemlett.9b00658

8)         Mo, C.; Zhang, Z.; Li, Y.; Huang, M.; Zou, J.; Luo, J.; Tu, Z.-C.; Xu, Y.; Ren, X.*; Ding, K.* and Lu, X. * Design and Optimization of 3'-(Imidazo[1,2-a]pyrazin-3-yl)-[1,1'-biphenyl]-3-carboxamides as Selective DDR1 Inhibitors. ACS Med. Chem. Lett. 2020, 11(3), 379-384.

9)         Xu, J.; Li, X.; Ding, K.*; Li, Z.* Applications of Activity-Based Protein Profiling (ABPP) and Bioimaging in Drug Discovery. Chemistry - An Asian J. 2020, 15(1), 34-41.

10)      Lu, X.*; Smail, J. B. Ding, K.* New Promise and Opportunities for Allosteric Kinase Inhibitors. New Promise and Opportunities for Allosteric Kinase Inhibitors. Angew. Chem. Int. Ed. 2020 https://doi.org/10.1002/anie.201914525

2019：

1)       Chang, Y.; Xu, S.; Ding, K.* Tyrosine Kinase 2 (TYK2) Allosteric Inhibitors To Treat Autoimmune Diseases. J. Med. Chem. 2019, 62, 8951-8952.

2)       Hu. X.; Xun, Q.; Zhang, T.; Li, Q.; Tang, L.; Lai, M.; Huang, T.; Yun, C.-H.*; Xie, H.*; Ding, K.*; and Lu, X.* 2-Oxo-3, 4-dihydropyrimido [4, 5-d] pyrimidines as new reversible inhibitors of EGFR C797S (Cys797 to Ser797) mutant. Chin. Chem. Lett. 2019, https://doi.org/10.1016/j.cclet.2019.09.044.

3)       Zhu, D.; Huang, H.; Pinkas, D. M.; Luo, J.; Ganguly,D; Fox, A. E.; Arner, E.; Xiang, Q.; Tu, Z.; Bukkock, A. N.* Brekken, R. A.* Ding, K.* Lu, X.* 2-Amino-2, 3-dihydro-1 H-indene-5-carboxamide-Based Discoidin Domain Receptor 1 (DDR1) Inhibitors: Design, Synthesis, and in Vivo Antipancreatic Cancer Efficacy. J. Med. Chem. 2019, 62, 7431-7444.

4)       Shen. J.; Zhang, T.; Zhu, S.-J.; Sun, M.; Tong, L.; Lai, M.; Zhang, R.; Xu, W.; Wu, R.; Ding, J.; Yun, C.-H.* Xie, H.* Lu, X.* Ding, K.* Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFRL858R/T790M/C797S). J. Med. Chem. 2019, 62, 7302-7308.

5)       Lin, X.; Yosaatmadja,Y.; Kalyukina, M.; Middleditch, M. J.; Zhang, Z.; Lu, X.; Ding, K.; Patterson, A. V.; Smaill, J. B.; Squire C. J. Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4. ACS Med. Chem. Lett. 2019, 10 (8), 1180-1186.

6)       Chang, Y.; Zhu, D.; Guo, H.; Yin, X.; Ding, K.; Li, Z.* Crenolanib‐Derived Probes Suitable for Cell‐and Tissue‐Based Protein Profiling and Single‐Cell Imaging. ChemBioChem 2019, 20 (14), 1783-1788.

7)       Cui, S.; Wang, Y.; Wang, Y.; Tang, X.; Ren, X.; Zhang, L.; Xu, Y.; Zhang, Z.*; Zhang, Z.*; Lu, X.*; Ding, K.* Design, synthesis and biological evaluation of 3-(imidazo [1, 2-a] pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitor. Eur. J. Med. Chem. , 2019, 179, 470-482.

8)       Xun, Z.; Wang, Z.; Hu, X.; Ding, K.*; Lu, X.* Small-Molecule CSF1R Inhibitors as Anticancer Agents. Curr. Med. Chem. 2019 doi: 10.2174/1573394715666190618121649.

9)       Yang, Z.; Shibu, M. A.; Kong. L.; BadrealamKhan, F.;  Luo, J.; Huang, Y.; Tu, Z.; Yun, C.*; Huang, C.-Y.*; Ding, K.*; Lu, X.* Design, Synthesis, and Structure–Activity Relationships of 1, 2, 3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitor. J. Med. Chem. 2019, https://doi.org/10.1021/acs.jmedchem.9b00664.

10)    Zou, J.; Zhang, Z.*; Xu, F.; Cui, S.; Qi, C.; Luo, J.; Wang, Z.; Lu, X., Tu, Z.; Re, X.; Song, Y.*, Ding, K.* GZD2202, a novel TrkB inhibitor, suppresses BDNF-mediated proliferation and metastasis in neuroblastoma models. J. Drug Targeting 2019, 27 (4), 442-450.

11)    Peng, L.*; Zhang, Z.; Lei, C.; Li, S.; Zhang, Z.; Ren, X.; Chang, Y.; Zhang, Y.; Xu, Y.; Ding, K.* Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation. ACS Med. Chem. Lett. 2019, 10, 767-772.

12)    Tang, L.; Zhang, Z.; Gao, D.; Chan, S.; Luo, J.; T. Z.; Zhang, Z.; Ding, K.*; Ren, X.*; Lu, X.* Eur. J. Med. Chem. 2019, 166, 318-327. 

13)     Zhang, Y.; Wang, Y.; Guo, Y.; Liao, J.; Tu, Z.; Lu, Y.; Ding, K.; Tortorella, M. D., He, J. Identification and synthesis of low-molecular weight cholecystokinin B receptor (CCKBR) agonists as mediators of long-term synaptic potentiation. Med. Chem. Res. 2019, 28, 387-393.

14)    Hu, X.; Wan, B.; Liu, Y.; Shen, J.; Franzblau, S. G.; Zhang, T.*; Ding, K.*; Lu, X. * Identification of Pyrazolo[1,5-a]pyridine-3-carboxamide Diaryl Derivatives as Drug Resistant Antituberculosis Agents. ACS Med. Chem. Lett. 2019, 10, 295-299.

15)    Ti, H.; Zhang, Y.; Liang, X.; Li, R.; Ding, K.*; Zhang, X.* Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). J. Med. Chem. 2019, 62, 5944-5978. 

16)    Liu, W.; Zhang, Z.; Zhang, Z.; Hao, P; Ding, K.; Li, Z. Integrated phenotypic screening and activity-based protein profiling to reveal potential therapy targets of pancreatic cancer. Chem. Comm. 2019, 55 (11), 1596-1599.

17)    Wang, X.; Ma, N.; Wu, R.; Ding, K., Li, Z. A novel reactive turn-on probe capable of selective profiling and no-wash imaging of Bruton's tyrosine kinase in live cells. Chem. Comm. 2019, 55 (24), 3473-3476.

18)  Guo, C.; Chang, Y.; Wang, X.; Zhang, C.; Hao, P.; Ding, K.; Li, Z. Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening. Chem. Comm. 2019, 55 (6), 834-837.

2018

1.    Xun, Q.; Zhang, Z.; Luo, J.; Tong, L.; Huang, M.; Wang, Z.; Zou, J.; Liu, Y.; Xu, Y.; Xie, H.; Tu, Z.-C.; Lu, X.* and Ding, K.* Design, Synthesis, and Structure–Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5-d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors. J. Med. Chem. 2018, 61, 2353–2371.

2.    Vasta, J. D.; Corona, C. R.; Wilkinson, J.; Zimprich, C. A.; Hartnett, J. R.; Ingold, M. R.; Zimmerman, K.; Machleidt, T.; Kirkland, T. A.; Huwiler, K.G.; Ohana, R. F.; Slater, M..; Otto, P.; Cong, M.; Wells, C. I.; Berger, B.-T.; Hanke, T.; Glas, C.; Ding, K.; Drewry, D. H.; Huber, K. V. M.; Willson, T. M.; Knapp, S.; Müller, S..; Meisenheimer, P. L.; Fan, F.; Wood, K. V.; Robers, M. B.*Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement. Cell Chem. Biol. 2018, 25, 206-214.e11.

3.    Xiang, Q.; Wang, C.; Zhang, Y.; Xue, X.; Song, M.; Zhang, C.; Li, C.; Wu, C..; Li, K.; Hui, X.; Zhou, Y.; Smaill, J. B.; Patterson, A. V.; Wu, D.; Ding, K.; Xu, Y.* Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer. Eur. J. Med. Chem. 2018, 147, 238-252.

4.    Xiang, Q.; Zhang, Y.; Li, J.; Xue, X.; Wang, C.; Song, M.; Zhang, C.; Wang, R.; Li, C.; Wu, C.; Zhou, Y.; Yang, X.; Li, G.; Ding, K.; Xu, Y.* Y08060: A Selective BET Inhibitor for Treatment of Prostate Cancer. ACS Med. Chem. Lett. 2018, 9, 262-267.

5.             Zhang, M.; Zhang, Y.; Song, M.; Xue, X.; Wang, J.; Wang, C.; Zhang, C.; Li, C.; Xiang, C.; Zou, L.; Wu, X.; Wu, C.; Dong, B.; Xue, W.; Zhou, Y.; Chen, H.; Wu, D.; Ding, K.; and Xu, Y.* Structure-Based Discovery and Optimization of Benzo[d]isoxazole Derivatives as Potent and Selective BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC). J. Med. Chem.2018, 61 (7), 3037-3058

6.    Zhang, Z.; Zou, J.; Yu, L.; Lou, J.; Li,Y.; Tu, Z.; Ren, X.; Wei, H.*; Song, L.*; Lu, X.*; Ding, K.* YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFR^{L858R, T790M}‐mutant resistance in vitro and in vivo. Cancer Medicine 2018, 7(4), 1430-1439.

7.            Zhu, D.; Guo, H.; Chang, Y.; Ni, Y.; Li, L.; Hao, P.;* Xu, Y.;Ding, K.;* and Li, Z.*  Cell- and Tissue-based Proteome Profiling and Dual Imaging of Apoptosis Markers with Probes Derived from Venetoclax and Idasanutlin. Angew Chem. Int. Ed. 2018, 57 (30), 9284-9289.

8.           Lu, X.; Williams, Z.; Hards, K.; Tang, J.; Cheung, C.-Y.; Aung, H. L.; Wang, B.; Liu, Z.; Hu, X.; Lenaerts, A.; Woolhiser, L.; Hastings, C.; Zhang, X.; Wang, Z.; Rhee, K.; Ding, K.; Zhang, T.; Cook, G. M. Pyrazolo[1,5-a]pyridine Inhibitor of the Respiratory Cytochrome bcc Complex for the Treatment of Drug-Resistant Tuberculosis. ACS Infectious Diseases 2018, 5 (2), 239-249.

9.           Lu, X. Chen, H.; Patterson, A. V.; Smaill, J. B.; Ding, K. Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects: Miniperspective. J. Med. Chem. 2018, 62 (6), 2905-2915.

10.        Lu, X.*; Zhang, T.; ZhU, S.; Xun, Q.; Tong, L.; Hu, X.; Li, Y.; Chan, S.; Su; Y.; Sun, Y.; Chen, Y.; Ding, J.; Yun, C.*; Xie, H.*; Ding, K.*  Discovery of JND3229 as a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy. ACS Med. Chem. Lett. 2018, 9 (11), 1123-1127.

11.        Zheng, B.; Guo, H.; Ma, N.; Ni, Y.; Xu, J.; Li, L.; Hao, P.; Ding, K.; Li, Z. Cell‐and Tissue‐Based Proteome Profiling and Bioimaging with Probes Derived from a Potent AXL Kinase Inhibitor. Chemistry–An Asian J. 2018, 13 (18), 2601-2605.

12.        Liu, Y.; Wang, Y.; Lu, X.; Tong, L.; Li, Y.; Zhang, T.; Xun, Q.; Feng, F.; Chen, Y.; Su, Y.; Shen, Y.; Chen, Y.; Geng, M.; Ding, K.; Li Y.; Xie, H.; Ding, J. Identification of compound D2923 as a novel anti-tumor agent targeting CSF1R. Acta pharmacologica Sinica 2018, 39 (11), 1768.

13.        Lu, X.*; Yu, L.; Zhang, Z.; Ren, X.; Smail, J. B.; Ding, K.* Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry. Med. Res. Rev. 2018, 38 (5), 1550-1581.

14.        Lei, C.; Peng, L.*; Ding, K.* Manganese‐Catalyzed C− H Annulation of Ketimines with Allenes: Stereoselective Synthesis of 1‐Aminoindanes. Adv. Syn. & Catal. 2018, 360 (15), 2952-2958.

15.            Wang, Z.; Zhang, Y.; Pinkas, D. M.; Fox, A. F.; Luo, J.; Huang, H.; Cui, S.; Xiang, Q.; Xu, T.; Xun, Q.; Zhu, D.; Tu. Z.; Ren, X.; Brekken,R. A.; Bullock, A. N.*; Liang, G.*; Ding, K.*; Lu, X.* Design, Synthesis, and Biological Evaluation of 3-(Imidazo [1, 2-a] pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin -1-yl) methyl)-5-(trifluoromethyl) phenyl) benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2. J. Med. Chem. 2018, 61, 7977-7990.

2017

1.    Wang, Z.; Zhang, Y.; Bartual, S. G.; Luo, J.; Xu, T.; Du, W.; Xun, Q.; Tu, Z.; Rolf A. Brekken, R. A.; Ren, X.; Bullock, A. N.*; Liang, G.*; Lu, X.*; and Ding, K. * Tetrahydroisoquinoline-7-carboxamide Derivatives as New Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. ACS Med. Chem. Lett., 2017, 8 (3), 327–332.

2.    Yang, J.; Tu, Z.; Xu, X.; Luo, J.; Yan, X.; Ran, C.; Mao, X.; Ding, K.*; Qiao, C.* Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents. Bioorg. Med. Chem. Lett. 2017, 27, 1341-1345.

3.    Jin, B.; Wang, C.; Li, J.; Du, X.; Ding, K.; Pan, J. Anthelmintic niclosamide disrupts the interplay of p65 and FOXM1/β-catenin and eradicates leukemia stem cells in chronic myelogenous leukemia. Clin. Cancer Res. 2017, 23, 789-803.  

4.    Lu, X.;* Tang, J.; Cui, S.; Wan, B.; Franzblauc, S.G.; Zhang, T.; Zhang, X.; Ding, K. Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity. Eur. J. Med. Chem. 2017, 125, 41-48.

5.    Mao, L.; Nie, B.; Nie, T.; Hui, X.; Gao, X.; Lin, X.; Liu, X.; Xu, Y.; Tang, X.; Yuan, R.; Li, K.; Li, P.; Ding, K.; Wang, Y.; Xu, A.; Fei, J.; Han, W.; Liu, P.; Madsen, L.; Kristiansen, K.; Zhou, Z.; Ding, S.; Wu, D. Visualization and quantification of browning using a Ucp1-2A-luciferase knock-in mouse model. Diabetes 2017, 66, 407-417.

6.    Hur, H.; Ham, I.-H.; Lee, D.; Jin, H.; Aguilera, K.Y.; Oh, H.J.; Han, S.-U.; Kwon, J. E.; Kim, Y.-B.; Ding, K.; Brekken, R. A. Discoidin domain receptor 1 activity drives an aggressive phenotype in gastric carcinoma. BMC Cancer 2017, 17, 17:87, DOI: 10.1186/s12885-017-3051-9.

7.    Yu, L.; Huang, M.; Xu, T.; Tong, L.; Yan, X.-E.; Zhang, Z.; Xu, Y.; Yun, C.; Xie, H.; Ding, K.*; Lu, X.* A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties. Eur. J. Med. Chem. 2017, 126, 1107-1117.

8.    Mo, C.; Zhang, Z.; Guise, C. P.; Li, X.; Luo, J.; Tu, Z.-C.; Paterson, A. V.; Smaill, J. B.;* Ren, X.;* Lu, X.;* and , Ding, K.* 2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors. ACS Med. Chem. Lett., 2017, 8(5), 543-548.

9.     Guo, H.; Xu, J.; Hao, P.*; Ding, K.*; Li, Z.* Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid. Chem. Comm. 2017, 53, 9620-9623.

10.   Chang, Y.; Lu, X.; Shibu, M.-A.; Dai, Y.-B.; Luo, J.; Zhang, Y.; Li, Y.; Zhao, P.; Zhang, Z.; Xu, Y.; Xu, Yong; Tu, Z.-C.; Zhang, Q.-W.*; Yun, C.-H.*; Huang, C.-Y.*; Ding, K.* Structure Based Design of N-(3-(1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-αMotif Kinase (ZAK) Inhibitors. J. Med. Chem. 2017, 60(13), 5927-5932.

11.  Li, X.; Guise, C. P.; Taghipouran, R.; Yosaatmadja, Y.; Ashoorzadeh, A.; Paik, W.-K.; Squire, C. J.; Jiang, S.; Luo, J.; Xu, Y.; Tu, Z.-C.; Lu, X.; Ren, X.; Patterson, A. V.; Smaill, J. B.*; Ding, K.* 2-Oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors. Eur. J. Med. Chem. 2017, 135, 531-543.

12.  Aguilera, K. Y.; Huang, H.; Du, W.; Hagopian, M. M.; Wang, Z.; Hinz, S.; Hwang, T. H.; Wang, H.; Fleming, J. B.; Castrillon, D. H.; Ren, X.; Ding, K.; and Brekken, R. A. Inhibition of discoidin domain receptor 1 reduces collagen-mediated tumorigenicity in pancreatic ductal adenocarcinoma. Mol. Cancer Ther. 2017, DOI:10.1158/1535-7163.MCT-16-0834.

13.  Cheng, K.; Lee, J.-S.; Yao, S. Q.; Ding, K* and Li, Z. * Tetrazole-based Photoprobes Enable Integration of Phenotypic Screening with Target Identification, and Distinct Profiling of a Cancer Biomarker. Angew Chem. Int. Ed. 2017, DOI:10.1002/anie.201709854

2016

1.    Wang, Z.; Bian, H.; Bartual, S. G.; Du, W.; Luo, J.; Zhao, H.; Zhang, S.; Mo, C.; Zhou, Y.; Xu, Y.; Tu, Z.; Ren, X.; Lu, X.; Brekken, R. A.; Yao, L.; Bullock, A. N.*; Su, J.* and Ding, K.* Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J. Med. Chem. 2016, 59, 5911–5916. (cover story)

2.    Tan, L.; Zhang, Z.; Gao, D.; Luo, J.; Tu, Z.-C.; Li, Z.; Peng, L.; Ren, X.*; and Ding, K.* 4-Oxo-1, 4-Dihydroquinoline-3-Carboxamide Derivatives as New Axl Kinase Inhibitors. J. Med. Chem. 2016, 59(14), 6807-25.

3.    Zou, Y.; Xiao, J.; Tu, Z.; Zhang, Y.; Yao, K.; Luo, M.; Ding, K.*; Zhang, Y.*; and Lai, Y.* Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors. Bioorg. Med. Chem. Lett. 2016, 26(13), 3052-3059.

4.    Li, X.; Shen, J.; Tan, L.; Zhang, Z.; Gao, D.; Luo, J.; Cheng, H.; Zhou, X.; Ma, J.*; Ding, K.*; and Lu, X.* Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors. Bioorg. Med. Chem. Lett. 2016, 26(12), 2760-2763.

5.    Shen, J.; Li, X.; Zhang, Z.; Luo, J.; Long, H.; Tu, Z.; Zhou, X.; Ding, K.* Lu, X.* 3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors. Chem. Biol. & Drug Design 2016, 690-698.

6.    Zhang, Z.; Ren, X.; Lu, X.; Wang, D.; Hu, X.; Zheng, Y.; Song, L.; Pang, H.; Yu, R.; and Ding, K.* GZD856, a novel potent PDGFRα/β inhibitor, suppresses the growth and migration of lung cancer cells in vitro and in vivo. Cancer Lett. 2016, 375(1), 172-178.

7.    Xue, X.;, Zhang, Y.; Liu, Z.; Song, M.; Xing, Y.; Xiang, Q.; Wang, Z.;, Tu, Z.; Zhou, Y.; Ding, K. and Xu, Y.* Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation..J. Med. Chem. 2016, 59(4), 1565-1579.

8.    Sang, F.; Ding, Y.; Wang, J.; Sun, B.; Sun, J.; Geng, Y.; Zhang, Z.; Ding, K.; Wu, L.-L.; Liu, J.-W.; Bai, C.; Yang, G.; Zhang, Q.; Li, L.-Y.; Chen, Y. Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. J. Med. Chem. 2016, 59(3), 1184-1196.

9.    Ambrogio, C.; Gómez-López, G.; Falcone, M.; Vidal, A.; Nadal, E.; Crosetto, N.; Blasco, R.-B.; Fernández-Marcos, P.-J.; Sánchez-Céspedes, M.; Ren, X.; Wang, Z.; Ding, K.; Hidalgo, M.; Serrano, M.; Villanueva, A.; Santamaría, D.; Barbacid, M. Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma. Nature Med. 2016, 22(3), 270-277.

10.  Ai, Y.; Zhu, B.;, Ren, C.; Kang, F.; Li, J.; Huang, Z.; Lai, Y.; Peng, S.; Ding, K.; Tian, J.; Zhang, Y. Discovery of New Monocarbonyl Ligustrazine-Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer. J. Med. Chem. 2016, 59(5), 1747-1760.

11.  Ye, W.; Jiang, Z.; Lu, X.; Ren, X.; Deng, M.; Lin, S.; Xiao, Y.; Lin, S.; Wang, S.; Li, B.; Zheng, Y.; Lai, P.; Weng, J.; Wu, D.; Ma, Y.; Chen, X.; Wen, Z.; Chen, Y.; Feng, X.; Li, Y.; Liu, P.; Du, X.; Pei, D.; Yao, Y.; Xu, B.; Ding, K.* and Li, Peng.* GZD824 suppresses the growth of human B cell precursor acute lymphoblastic leukemia cells by inhibiting the SRC kinase and PI3K/AKT pathways. Oncotarget 2016, doi: 10.18632/oncotarget.10881.

2015

1.     Li, Y.; Lu, X.; Ren X..*, and Ding, K*. Small Molecule Discoidin Domain Receptor Kinase Inhibitors and Potential Medical Applications. J. Med. Chem. 2015, 58(8), 3287-3301.

2.    Yu, L.; Wang, Z.; Zhang Z.; Ren. X.; Lu X.*; Ding, K.* Small-Molecule BET Inhibitors in Clinical and Preclinical Development and Their Therapeutic Potential. Curr. Top. Med. Chem. 2015, 15(8), 776-794.

3.    Li, Y.; Cheng, H.; Zhang, Z.; Zhuang, X.; Luo, J.; Long, H.; Zhou, Y.; Taghipouran, R.; Li, D.; Patterson, A.; Smaill, J.; Tu, Z.; Wu, D.; Ren, X.*; Ding, K.* N- -(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors. ACS Med. Chem. Lett. 2015, 6(5), 543-547.

4.    Xu, S.; Mao, L.; Ding, P.; Zhuang, X.; Zhou, Y.; Yu, L.; Liu, Y.; Nie, T.; Xu, T.; Xu, Y.; Liu, J.; Smaill, J.; Ren, X.*; Wu, D.*; & Ding, K.* 1-Benzyl-4-Phenyl-1H-1,2,3-Triazoles Improve the Transcriptional Functions of Estrogen-Related Receptor γ and Promote the Browning of White Adipose. Bioorg. Med. Chem. 2015, 23(13), 3751-3760.

5.    Tang, J.; Wang, B.; Wu, T.; Wan, J.; T. Z.; Njire, M.; Wan, B.; Franzblau, S. M.; Zhang, T.*; Lu, X.*; and Ding, K.* Design, Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Anti-tubercular Agents. ACS Med. Chem. Lett. 2015, 6(7), 814-816.

6.    Chan, S.; Han, K.; Qu, R.; Tong, L.; Li, Y.; Zhang, Z.; Cheng, H.; Lu, X.; Patterson, A.; Smaill, J.; Ren, X.; Ding, J.; Xie, H.* and Ding, K.* 2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR^(L⁸⁵⁸^R/T⁷⁹⁰^M). Bioorg. Med. Chem. Lett.. 2015, 25(19), 4277-4281.

7.    Lu, X.; Zhang, Z.; Ren, X.; Pan, X.; Wang, D.; Zhuang, X.; Luo, J.; Yu, R. and Ding, K.* Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl^(T315I) mutant. Bioorg. Med. Chem. Lett. 2015, 25(17), 3458-3463.

8.    Qin, J.; Ji, J.; Deng, R.; Tang, J.; Yang, F.; Feng, G.-K.; Chen, W.-D.; Wu, X.-Q.; Qian, X.-J.; Ding, K.* and Zhu, X.-F.* DC120, a novel AKT inhibitor, preferentially suppresses nasopharyngeal carcinoma cancer stem-like cells by downregulating Sox2. Oncotarget. 2015, 6(9), 6944-6958.

2014.

1.        Cheng, H.; Chang, Y.; Zhang, L.; Luo, J.; Tu, Z.; Lu, X.; Zhang, Q.; Ren, X. and Ding, K.* Identification and Optimization of New Dual Inhibitors of B-Raf and Epidermal Growth Factor Receptor Kinases for Overcoming Resistance against Vemurafenib. J. Med. Chem. 2014, 57, 2692–2703.

2.        Lu, X. and Ding, K.* Novel Anaplastic Lymphoma Kinase Inhibitors Targeting Clinically Acquired Resistance. J. Med. Chem. 2014, 57, 1167-1169.

3.    Yang, Y.; Deng, R.; Qian, X,-J.; Chang, S.-H.; Wu, X.-Q.; Qin, J.; Feng, G.-K.; Ding, K.*; and Zhu, X.-F.*. Feedback Loops Blockade Potentiates Apoptosis Induction and Antitumor Activity of a Novel AKT Inhibitor DC120 in Human Liver Cancer. Cell Death and Disease 2014, 5, doi:10.1038/cddis.2014.43.

4.    Shen, Y.; Ren, X.; Ding, K.; Zhang, Z.; Wang, D.; Pan, J. Antitumor activity of S116836, a novel tyrosine kinase inhibitor, against imatinib-resistant FIP1L1-PDGFRα-expressing cells. Oncotarget. 2014, 5(21):10407-20.

5.    Wang, W.; Kong, D.; Cheng, H.; Tan, L.; Zhang, Z.; Zhuang, X.; Long, H.; Zhou, Y.; Xu, Y.; Yang, X.* and Ding, K.* New benzimidazole-2-urea derivates as tubulin inhibitors. Bioorg Med Chem Lett. 2014, 24(17): 4250-3.

6.    Bu Q, Cui L, Li J, Du X, Zou W, Ding K, Pan J. SAHA and S116836, a novel tyrosine kinase inhibitor, synergistically induce apoptosis in imatinib-resistant chronic myelogenous leukemia cells. Cancer Biol Ther. 2014, 15(7), 951-62.

7.    Han C, Wan L, Ji H, Ding K, Huang Z, Lai Y, Peng S, Zhang Y. Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. Eur J Med Chem. 2014, 77, 75-83.

8.    Jin B, Ding K, Pan J. Ponatinib induces apoptosis in imatinib-resistant human mast cells by dephosphorylating mutant D816V KIT and silencing β-catenin signaling. Mol Cancer Ther. 2014, 13(5), 1217-30.

9.    Jin Y, Ding K, Li H, Xue M, Shi X, Wang C, Pan J. Ponatinib efficiently kills imatinib-resistant chronic eosinophilic leukemia cells harboring gatekeeper mutant T674I FIP1L1-PDGFRα: roles of Mcl-1 and β-catenin. Mol Cancer. 2014, 13, 17, DOI: 10.1186/1476-4598-13-17.

2013

1.    Xu, T.; Zhang, L.; Xu, S.; Yang, C-Y; Luo, J.; Ding, F.; Lu, X.*; Liu, Y.; Tu, Z.; Li, S.; Pei, D.; Cai, Q.; Li, H.; Ren, X.; Wang, S.; and Ding, K.*Pyrimido[4,5-d]pyrimidin-4(1H)-one derivatives as Selective Inhibitors of EGFR Threonine⁷⁹⁰→Methionine⁷⁹⁰ (T790M) Mutants. Angew. Chem. Int. Ed. 2013, 52, 8387–8390.

2.    Xu, S.; Xu, T.; Zhang, L.; Zhang, Z.; Luo, J.; Liu, Y.; Lu, X.; Tu, Z.; Ren, X.; Ding, K.*Design, Synthesis and Biological Evaluation of 2-Oxo-3,4-dihydropyrimido[4,5-d] pyrimidinyl Derivatives as New Irreversible Epidermal Growth Factor Receptor Inhibitors with Improved Pharmacokinetic Properties. J. Med. Chem. 2013, 56 (21), 8803–8813.

3.    Zhou, W.; Liu, X.; Tu, Z.; Zhang, L.; Ku, X.; Bai, F.; Zhao, Z.; Xu, Y.;* Ding, K.* and Li, H.* Discovery of pteridin-7(8H)-one-based Irreversible Inhibitors targeting Epidermal Growth Factor Receptor (EGFR) Kinase T790M/L858R mutant. J. Med. Chem. 2013, 56 (20), 7821–7837.

4.    Xu, S.; Zhuang, X.; Pan, X.; Zhang, Z.; Duan, L.; Liu, Y.; Zhang, L.; Ren, X.*and Ding, K.* 1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as Orally Bioavailable Transcriptional Function Suppressors of Estrogen-Related Receptor α. J. Med. Chem. 2013, 56 (11), 4631–4640.

5.    Ren, X.; Pan, X.; Zhang, Z.; Wang, D.; Lu, X.; Li, Y.; Wen, D.; Long, H.; Luo, J.; Feng, Y.; Zhuang, X.; Zhang, F.; Liu, J.; Leng, F.; Lang, X.; Bai, Y.; She, M.; Tu, Z.; Pan, J. and Ding, K. * Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and non-phosphorylated Bcr-Abl and overcomes clinically acquired mutation-induced resistance against imatinib. J. Med. Chem. 2013, 56(3):879-94 [Highlighted by SciBX (Science-Business eXchange), a translational journal in Nature publish group]

6.    Gao, M.; Duan, L.; Luo, J.; Zhang, L.; Lu, X.; Zhang, Y.; Zhang, Z.; Tu, Z.; Xu, Y.; Ren, X. and Ding, K. *Discovery and Optimization of 3-(2-(Pyrazolo[1,5-a] pyrimidin-6-yl)ethynyl)benzamides as Novel Selective and Orally Bioavailable Discoidin Domain Receptor 1 (DDR1) Inhibitors. J. Med. Chem. 2013, 56(3),879-894. [Highlighted by SciBX (Science-Business eXchange]

7.    Han, C.; Huang, Z.; Zheng, C.; Wan, L.; Zhang, L.; Peng, S.; Ding, K.*; Ji, H.*; Tian, J. and Zhang, Y.*Novel Hybrids of (Phenylsulfonyl)furoxan and Anilinopyrimidine as Potent and Selective Epidermal Growth Factor Receptor Inhibitors for Intervention of Non-Small-Cell Lung Cancer. J. Med. Chem. 2013, 56 (11), 4738–4748.

2012.

1.   Zhou, F.; Guo, J.; Liu, J.; Ding, K.; Yu, S.; Cai, Q. Copper-Catalyzed Desymmetric Intramolecular Ullmann C–N Coupling: An Enantioselective Preparation of Indolines. J. Am. Chem. Soc. 2012, 134 (35), 14326-14329.

2.   Zhang, J.; Zhou, J.; Ren, X.; Diao, Y.; Li, H.; Jiang, H.; Ding, K. *; Pei, D. A new diaryl urea compound, D181, induces cell cycle arrest in the G1 and M phases by targeting receptor tyrosine kinases and the microtubule skeleton. Invest. New Drugs 2012, 30 (2), 490-507.

3.   Yan, J.; Zhou, F.; Qin, D.; Cai, T.; Ding, K.; Cai, Q. Synthesis of [1,2,3]Triazolo[1,5-a]quinoxalin-4(5H)-ones through Copper-Catalyzed Tandem Reactions of N-(2-Haloaryl)propiolamides with Sodium Azide. Org. Lett. 2012, 14 (5), 1262-1265.

4.   Xu, S.; Zhang, L.; Chang, S.; Luo, J.; Lu, X.; Tu, Z.; Liu, Y.; zhang, Z.; Xu, Y.; Ren, X.; Ding, K.* Design, synthesis and biological evaluation of new molecules inhibiting epidermal growth factor receptor threonine790 → methionine790 mutant. MedChemComm 2012, 3 (9), 1155-1159.

5.   Wu, Y.; Chen, C.; Sun, X.; Shi, X.; Jin, B.; Ding, K.; Yeung, S.-C. J.; Pan, J. Cyclin-Dependent Kinase 7/9 Inhibitor SNS-032 Abrogates FIP1-like-1 Platelet-Derived Growth Factor Receptor α and Bcr-Abl Oncogene Addiction in Malignant Hematologic Cells. Clin. Cancer. Res. 2012, 18 (7), 1966-1978.

6.   Pan, J.; Ding, K.; Wang, C. Niclosamide, an old antihelminthic agent, demonstrates antitumor activity by blocking multiple signaling pathways of cancer stem cells. Chinese J. Cancer 2012, 31 (4), 178-184.

7.   Lu, X.; Peng, L.; Lv, M.; Ding, K. * Recent Advance in the Design of Small Molecular Modulators of Estrogen-Related Receptors. Curr. Pharm. Des. 2012, 18 (23), 3421-3431.

8.   Lu, X.; Lv, M.; Huang, K.; Ding, K.; You, Q. Pharmacophore and Molecular Docking Guided 3D-QSAR Study of Bacterial Enoyl-ACP Reductase (FabI) Inhibitors. Int. J. Mol. Sci. 2012, 13 (6), 6620-6638.

9.   Lin, W.; Huang, X.; Zhang, L.; Chen, D.; Wang, D.; Peng, Q.; Xu, L.; Li, J.; Liu, X.; Li, K.; Ding, K.; Jin, S.; Li, J.; Wu, D. BMS309403 Stimulates Glucose Uptake in Myotubes through Activation of AMP-Activated Protein Kinase. PLoS ONE 2012, 7 (8), e44570.

10. Li, Y.; Shen, M.; Zhang, Z.; Luo, J.; Pan, X.; Lu, X.; Long, H.; Wen, D.; Zhang, F.; Leng, F.; Li, Y.; Tu, Z.; Ren, X.; Ding, K. * Design, Synthesis, and Biological Evaluation of 3-(1H-1,2,3-Triazol-1-yl)benzamide Derivatives as Potent Pan Bcr-Abl Inhibitors Including the Threonine315→Isoleucine315 Mutant. J. Med. Chem. 2012, 55 (22), 10033-10046.

11. Deng, R.; Yang, F.; Chang, S.-h.; Tang, J.; Qin, J.; Feng, G.-K.; Ding, K.; Zhu, X.-F. DC120, a Novel and Potent Inhibitor of AKT Kinase, Induces Tumor Cell Apoptosis and Suppresses Tumor Growth. Mol. Pharmacol. 2012, 82 (2), 189-198.

12. Cheng, H.; Wan, J.; Lin, M.-I.; Liu, Y.; Lu, X.; Liu, J.; Xu, Y.; Chen, J.; Tu, Z.; Cheng, Y.-S. E.; Ding, K. * Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein. J. Med. Chem. 2012, 55 (5), 2144-2153.

13. Chang, S.; Zhang, L.; Xu, S.; Luo, J.; Lu, X.; Zhang, Z.; Xu, T.; Liu, Y.; Tu, Z.; Xu, Y.; Ren, X.; Geng, M.; Ding, J.; Pei, D.; Ding, K. * Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 → Methionine790 Mutant. J. Med. Chem. 2012, 55 (6), 2711-2723.

14. Cai, Q.; Yan, J.; Ding, K. * A CuAAC/Ullmann C–C Coupling Tandem Reaction: Copper-Catalyzed Reactions of Organic Azides with N-(2-Iodoaryl)propiolamides or 2-Iodo-N-(prop-2-ynyl)benzenamines. Org. Lett. 2012, 14 (13), 3332-3335.

2011

1. Peng, L.; Gao, X.; Duan L.; Ren, X.; Wu, D. and Ding, K. * Identification of Pyrido[1,2-α]pyrimidine-4-ones as New Molecules Improving the Transcriptional Functions of Estrogen-Related Receptor α. J. Med. Chem. 2011, 54, 7729–7733.

2. Cai, Q.; Zhou, F.; Xu, T.; Fu, L. and Ding, K. * Copper-Catalyzed Tandem Reactions of 1-(2-Iodoary)-2-yn-1-ones with Isocyaanides for the Synthesis of 4-Oxo-indeno[1,2-b]pyrroles. Organic Letters 2011, 13, 340-343.

3. Lu, X.; Cai, Q.; and Ding, K.* Recent Developments in the Third Generation Inhibitors of Bcr-Abl for Overriding T315I mutation. Current Medicinal Chemistry 2011, 18(14), 2146-57.

4. Zhou, F.; Liu, J.; Ding, K.; Liu, J. and Cai, Q. Copper-Catalyzed Tandem Reaction of Isocyanides with N-(2-Haloaryl) propiolamides for the Synthesis of Pyrrolo[3,2-c]quinolin-4-ones. J. Org. Chem. 2011, 76 (13), 5346-5353.

5. Liu, X.; Huang, X.; Wang, D.; Diao, Y.; Li, H.; Hui, Y.; Wang, Y.; Xu, A.; Wu, D.; Ding, K.*. New Aromatic Substituted Pyrazoles as Selective Inhibitors of Human Adipocyte Fatty Acid-Binding Protein. Bioorg. Med. Chem. Lett. 2011, 21, 2949-2952.

6. Peng, L.; Duang, L.; Liu, X.; Shen, M.; Li, Y.; Yan, J.; Li, H.; and Ding, K. * Structure–activity study on a series of α-glutamic acid scaffold based compounds as new ADAMTS inhibitors. Bioorg. Med. Chem. Lett. 2011, 21, 4457- 4461.

7. Wang, D.; Zhang, Z.; Lu, X.; Feng, Y.; Luo, K.; Gan, J.; Liu, Y.; Lu, J.; Li, X.; Zhang, F.; Tu, Z.; Cai, Q.; Ren, X.; and Ding, K.* Hybrid Compounds as New Bcr-Abl Inhibitors. Bioorg. Med. Chem. Lett. 2011, 21(7), 1965-1968.

8. Chen, J.; Liu, J.; Yang, J.; Chen, Y.; Chen, J.; Ni, S.; Song, H.; Zeng, L.;  Ding, K.; Pei, D. BMPs functionally replace Klf4 and support efficient reprogramming of mouse fibroblasts by Oct4 alone. Cell Research 2011, 21, 205-212.

9. Jiang, H.; Wang, X.; Huang, L.; Luo, Z.; Su, T.; Ding, K. * and Lin, X. * Benzenediol-berberine hybrids: Multifunctional agents for Alzheimer’s disease. Biorog. Med. Chem. 2011, 19, 7228-7235.

10. Gao, M.; Liu, X.; Wang, X.; Cai, Q.; and Ding, K. * Synthesis of 1-Aryl-1H-indazoles via a Ligand-Free Copper- Catalyzed Intramolecular Amination Reaction. Chinese J. Chem. 2011, 29, 1119-1204. （cited time:2）

11. Zhou, F.; Ding, K.* and Cai, Q. * Palladium-Catalyzed Amidation of N-Tosylhydrazones with Isocyanides. Chem., Eur. J. 2011, 17, 12268–12271.

2010

1. Ren, X.; He, Q.; Duan, L.; Zhang, Z.; Zhou, Y.; Wu, D.; pan, J. and Ding, K. *. Identification of a New Small-Molecule Inhibitor of STAT3 Signaling Pathway by Using a “Repositioning” Strategy. ACS Med. Chem. Lett. 2010, 2010, 1 (9), 454–459.

2. Cai, Q.; Wei, J.; Fu, L.; Pei, D.; and Ding, K. *. Synthesis of Aza-Fused Polycyclic Quinolines through Copper-Catalyzed Cascade Reactions. Org. Lett. 2010, 12(7): 1500-1503.

4. Chen, H.; Wang, D.; Wang, X.; Hung, W.; Cai, Q.; and Ding, K. * Mild Conditions for Copper-Catalyzed N-Arylation of Imidazoles. Synthesis 2010, 9, 1505-1511.

5. Li, Z.; Fu, L.; Wei, J.; Ha, C.; Pei, D.; Cai, Q. and Ding, K. * A Room-Temperature, Copper-Catalyzed Cascade Process for Diethyl 2-Aryl-3,4-dihydro-4-oxo-1,1(2H)-naphthalenedicarboxylate. Synthesis 2010, 9, 3289-3294.

6. Jin, Y.; Lu, Z.; Ding, K.; Li, J.; Du, X.; Chen, C.; Sun, X. Wu, Y.; Zhou, J.; and Pan, J. Antineoplastic Mechanisms of Niclosamide in Acute Myelogenous Leukemia Stem Cells: Inactivation of the NF- B Pathway and Generation of Reactive Oxygen Species. Cancer Res. 2010, 70, 2516-2527.

7. Hui, X.; Li, H.; Zhou, Z.; Lam, K. S. L.; Xiao, Y.; Wu, D.; Ding, K.; Wng, Y.; Vanhoutte, P. M.; Xu. A. Adipocyte Fatty Acid Binding Protein Modulates Inflammatory Responses in Macrophages through a Positive Feedback Loop Involving C-Jun N-terminal kinases and Activator Protein-1. J. Bio. Chem. 2010, 285, 10273-10280.

8. Shi, X.; Wang, D.; Ding, K.; Lu, Z.; Jin, Y.; Zhang, J.; and Pan, J. Pan.eGDP366, a novel small molecule dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells. Cancer Biolo&Therapy. 2010, 9, 640-650.

2009.

1. Wang, D.; and Ding, K. * 2-Pyridinyl beta-Ketones as New Ligands for Room-Temperature CuI-Catalysed C-N Coupling Reactions. Chem. Comm. 2009, 1891-1893.

2. Cai, Q.; Li, Z.; Wei, J.; Ha, C.; Pei, D.; and Ding, K.* Assembly of indole-2-carboxylic acid esters through a ligand-free copper-catalysed cascade process. Chem. Commun. 2009, 48, 7581-7583.

3. Wang, D.; Cai, Q. and Ding, K. * An Efficient Cu-Catalyzed Amination of Aryl Halides by Aqueous Ammonia. Adv. Synth. Catal. 2009, 351, 1722-1726.

4. Zhou, J.; Duan, L.; Chen, H.; Ren, X.; Zhang, Z.; Zhou, F.; Liu, J.; pei, D. and Ding, K.* Atovaquone Derivatives as Potent Cytotoxic and Apoptosis Inducing Agents. Bioorg. Med. Chem. Lett. 2009, 19, 5091-5094.

5. Zhang, Q.; Wang, D.; Wang, X.; and Ding, K.* (2-Pyridyl)acetone Promoted Cu-Catalyzed O-arylation of Phenols with Aryl Iodides, Bromides and chlorides. J. Org. Chem. 2009, 74, 7187-7190.

6. Yu, S.; Qin, D.; Shangary, S.; Chen, J.; Wang, G.; Ding, K.; McEachern, D.; Qiu, S.; Nikolovska-Coleska, Z.; Miller, R.; Kang, S.; Yang, D. and Wang, S. Potent and Orally Active Small-Molecule Inhibitors of the MDM2-p53 Interaction. J. Med. Chem. 2009, 7970-7973.

7. Canner, J. A.; Sobo, M.; Ball, S.; Hutzen, B.; DeAngelis, S.; Willis, W.); Studebaker, A. W.; Ding, K.; Wang, S.; Yang, D..; Lin, J. MI-63: A novel small-molecule inhibitor targets MDM2 and induces apoptosis in embryonal and alveolar rhabdomyosarcoma cells with wild-type p53. British J. Cancer 2009, 101,774-781.

2008

1. Sun, S. H.; Zheng, M.; Ding, K.; Wang, S.; Sun, Y. A small molecule that disrupts Mdm2-p53 binding activates p53, induces apoptosis and sensitizes lung cancer cells to chemotherapy. Cancer Biology & Therapy 2008, 7, 845-852.

2. Wang, D.; Kuang, L.; Li, Z.; Ding, K.* L-proline Promotes Rosenmund-Von Braun Reaction. SynLett 2008, 69-72.

3. Wang, G.; Zhang, H.; Zhou, J.; Ha, C.; Pei, D. and Ding, K*. An Efficient Synthesis of ABT-263, a Novel Inhibitor of Anti-apoptotic Bcl-2 Proteins. Synthesis 2008, 15, 2398 - 2404.

4. Zhou, J.; Fu, L.; Lv, M.; Liu, J.; Pei, D. and Ding, K.* Ligand Free  CuI-Catalyzed Domino Process to Quinazolin-4(3H)-ones. Synthesis 2008, 3974-3980.

5. Wang, G, Li, Z, Ha, C, Ding, K*. Direct oxidation of N-benzylamides to aldehydes or ketones by N-bromosuccinimide. Synthetic Communications 2008, 38, 1629-1637.

6. Shangary, S.; Qin, D.; McEachern, D.; Liu, M.; Miller, R. S.; Qiu, S.; Nikolovska-Coleska, Z.; Ding, K.; Wang, G.; Chen, J.; Bernard, D.; Zhang, J.; Lu, Y.; Gu, Q.; Shah, R. B.; Pienta, K. J.; Ling, X.; Kang, S.; Guo, M.; Sun, Y.; Yang, D.; Wang, S. Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition. Proceedings of the National Academy of Sciences of the United States of American 2008, 105, 3933-3938.

7. Shangary, S.; Ding, K.; Qiu, S.; Nikolovska-Coleska, Z.; Bauer, J. A.; Liu, M.; Wang, G.; Lu, Y.; McEachern, D.; Bernard, D.; Bradford, C. R.; Carey, T. E.; Wang, S. Reactivation of p53 by a specific MDM2 antagonist (MI-43) leads to p21-mediated cell cycle arrest and selective cell death in colon cancer. Molecular Cancer Therapeutics 2008, 7, 1533-1542.

8. Jiang, S.; Li, Z.; Ding, K.; Roller, P. P. Recent progress of synthetic studies to peptide and peptidomimetic cyclization. Current Organic Chemistry 2008, 12, 1502-1542.

9. Sun, S. H.; Zheng, M.; Ding, K.; Wang S.; Sun Y. A small molecule that disrupts Mdm2-p53 binding activates p53, induces apoptosis, and sensitizes lung cancer cells to chemotherapy. Cancer Biol Ther. 2008, 7, 845 – 852.

2007

1. Kuang, L.; Zhou, J.; Chen, S.; Ding, K.* Room-Temperature Debenzylation of N-Benzylcarboxamides by N-Bromosuccinimide. Synthesis 2007, 3129 - 3134.

2. Tang, G.; Ding, K.; Nikolovska-Coleska, Z.; Yang, C.-Y.; Qiu, S.; Shangary, S.; Wang, R.; Guo, J.; Gao, W.; Meagher, J.; Stuckey, J.; Krajewski, K.; Jiang, S.; Roller, P. P. and Wang, S. Structure-Based Design of Flavonoid Compounds As a New Class of Small-Molecule Inhibitors of the Anti-apoptotic Bcl-2 Proteins. J. Med. Chem. 2007, 50, 3163-3166.

3. Zhang, M.; Ling, Y.; Yang, C.-Y.; Liu, H.; Wang, R.; Wu, X.; Ding, K, Zhu, F.; Griffith, B. N.; Mohammad, R. M.; Wang, S.; Yang, D. A novel Bcl-2 small molecule inhibitor 4-(3-methoxy-phenylsulfannyl) -7-nitro-benzo furazan-3-oxide (MNB)–induced apoptosis in leukemia cells. Ann Hematol. 2007, 86, 471-81.

2006

1. Ding, K.; Lu, Y.; Nikolovska-Coleska, Z.; Wang, G.; Qiu, S.; Shangary, S.; Gao, W.; Qin, D.; Stuckey, J.; Krajewski, K.; Roller, P. P. and Wang, S. Structure-Based Design of Spiro-oxindoles as Potent, Specific Small-Molecule Inhibitors of the MDM2-p53 Interaction. J. Med. Chem. 2006, 49, 3432-3435.

2. Ma, D.; Jiang, Y.; Chen, F.; Gong, L.-K.; Ding, K.; Xu, Y.; Wang, R.; Ge, A.; Ren, J.; Li, J.; Li, J. and Ye, Q. Selective Inhibiton of Matrix Metalloproteinase Isozyme and In Vivo Protection SAainst Emphysema by Substituteb γ-Keto Carboxylic Acids. J. Med. Chem. 2006, 49, 456-458.

3. Chen, J.; Ding, K.; Levant, B.; and Wang, S. Design of Novel Hexahydropyrazinoquinoline as potent and selective dopamine D3 receptor with improved solubility. Bioorg. & Med.Chem. Letts. 2006, 16, 443-446.

2005

1. Ding, K.; Lu, Y.; Nikolovska-Coleska, Z.; Qiu, S.;  Ding, Y.; Stuckey, J.; Roller, P. P.; Tomita, Y.; Deschamps, J. R. and Wang, S. Structure-Based Design of Potent and Non-Peptide Small-Molecule Inhibitors of the p53-MDM2 Interaction. J. Am. Chem. Soc. 2005, 127, 10130-10131.

2. Ding, K.; Chen, J.; Ji, M.; Wu, X.; Varady, J.; Levant, B. and Wang, S. Design, synthesis and evaluation of enantiomerically pure substituted hexahydropyrazinolines as potent and highly selective Dopamine 3 receptor ligands. J. Med. Chem. 2005, 48, 3171-3181.

3. Ding, K.; Wang, G.; Deschamps, J. R.; and Wang, S. Spirooxindoles via asymmetric 1,3-dipolar cycloaddition. Tetrahedron Letters. 2005, 46, 5949-5951.

4. Ding, K. and Wang, S. An Efficient synthesis of isoflavone analogues via a Suzuki coupling reaction. Tetrahedron Letters 2005, 46, 3707-3709. 

硕士研究生 有机化学（药物化学）
博士研究生 有机化学（药物化学）