杨春皓-中国科学院大学-UCAS

基本信息

杨春皓男汉族博导上海药物研究所
电子邮件：chyang@mail.shcnc.ac.cn
联系电话：
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通信地址：
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研究领域

抗肿瘤药物、抗骨质疏松药物、具有生物活性的新型杂环及其合成方法学

招生信息

招生专业

100701-药物化学

招生方向

药物合成化学
药物合成化学

教育背景

1988-1992    苏州大学化学系
1992-1995  华东师范大学化学系
2000-2003  上海药物研究所

学历

-- 研究生

学位

-- 博士

出国学习工作

2008.8-2009.1 Georgia State University

教授课程

Medicinal Chemistry

专利与奖励

专利成果

[1] 高召兵, 杨春皓, 谭村, 郑月明, 符琳书, 许海燕, 张小飞, 陈笑艳, 胡有洪, 熊兵, 贺茜, 魏爱环. 脒类衍生化合物及其制备方法和用途. CN: CN116655497A, 2023-08-29.
[2] 高召兵, 胡有洪, 魏爱环, 郑月明, 杨春皓, 熊兵, 陈笑艳, 秦慧, 谭村, 许海燕, 周雷. 酰胺类化合物及其制备方法和用途. 202210267217.3, 2022-03-17.
[3] 杨春皓, 左建平, 王洁, 何世君, 张小飞, 林泽民. 含吡唑的白桦脂酸类衍生物，其制备方法及用途. CN: CN114805469A, 2022-07-29.
[4] 谢山山, 杨春皓, 张小飞, 谭村. 吡咯霉素衍生物的制备方法及其中间体. CN: CN113527170A, 2021-10-22.
[5] 杨春皓, 李群益, 代天资, 漆学宇, 谭村, 陈海飞, 张留弟. 取代噻吩类化合物、其制备方法及其用途. CN: CN112142711B, 2022-03-29.
[6] 沈孝坤, 杨春皓. 盐酸美呋哌瑞多晶型物及其制备方法. CN: CN111320596A, 2020-06-23.
[7] 江敏, 彭蕾, 王天骐, 徐醒, 杨春皓, 邓廉夫. 一类DL-色氨酸类化合物、其制备方法及用途. CN: CN111170923A, 2020-05-19.
[8] 江敏, 彭蕾, 王天骐, 徐醒, 杨春皓, 邓廉夫. 一类DL-色氨酸类化合物、其制备方法及用途. CN: CN111170923B, 2023-07-25.
[9] 杨春皓, 彭小峰, 张小飞, 谭村, 鲁云福, 蓝乐夫. 5-（2-羟基苯甲酰基）吡唑类化合物及其制备方法与应用. CN: CN110878051A, 2020-03-13.
[10] 杨春皓, 彭小峰, 张小飞, 谭村, 鲁云福, 蓝乐夫. 5-（2-羟基苯甲酰基）吡唑类化合物及其制备方法与应用. CN: CN110878051B, 2023-01-24.
[11] 阳华, 向皞月, 赵庆兰, 杨春皓. 一种喹诺酮骨架及其合成方法. CN: CN108929267B, 2021-07-02.
[12] 谭村, 张小飞, 杨春皓, 缪泽鸿, 宋姗姗, 宦霞娟, 陈奕, 丁健. 酞嗪酮类衍生物、其制备方法和用途. CN: CN110194762A, 2019-09-03.
[13] 杨春皓, 缪泽鸿, 陈建阳, 宦霞娟, 丁健, 陈奕, 谭村, 贺茜. 吡咯[1,2-b]哒嗪类化合物或其可药用盐及它们的用途. CN: CN109232575B, 2022-01-25.
[14] 杨春皓, 缪泽鸿, 陈建阳, 宦霞娟, 丁健, 陈奕, 谭村, 贺茜. 吡咯1,2-b哒嗪类化合物或其可药用盐及它们的用途. CN: CN109232575A, 2019-01-18.
[15] 杨春皓, 蒙凌华, 向皞月, 李京, 王祥, 谭村, 贺茜, 丁健, 陈奕. 7-位取代吡咯并三嗪类化合物或其药学上可用的盐，及其制备方法和用途. CN: CN109111447A, 2019-01-01.
[16] 杨春皓, 缪泽鸿, 谭村, 宦霞娟, 丁健, 陈奕. 盐酸美呋哌瑞多晶型物及其制备方法与应用. CN: CN109134409A, 2019-01-04.
[17] 江敏, 徐醒, 邓廉夫, 姜波, 杨春皓. 一类大黄酸硫代酰胺类化合物、其制备方法及用途. CN: CN107298648A, 2017-10-27.
[18] 杨春皓, 缪泽鸿, 陈旭星, 宦霞娟, 王玉勤, 谭村, 陈奕. 2-取代苯并咪唑-4-甲酰胺类化合物及制备方法和应用. CN: CN107922430B, 2020-09-04.
[19] 杨春皓, 缪泽鸿, 陈旭星, 宦霞娟, 王玉勤, 谭村, 陈奕, 丁健. 2‑取代苯并咪唑‑4‑甲酰胺类化合物及制备方法和应用. CN: CN107922430A, 2018-04-17.
[20] 江敏, 徐醒, 漆学宇, 杨春皓, 邓廉夫. 一类大黄酸类化合物及其用途. CN: CN105884645A, 2016-08-24.
[21] 杨春皓, 缪泽鸿, 张小飞, 衣君玫, 贺茜, 宦霞娟, 宋姗姗, 王迎庆, 陈奕, 丁健. α-咔啉类化合物，其制备方法以及用途. CN: CN105820165A, 2016-08-03.
[22] 杨春皓, 邵吉民, 朱维良, 徐志建, 王猛, 陈新焕, 侯传伟, 刘霞, 李波, 陈凯先. 取代酰胺苯酚类化合物及其制备方法、药物组合物和用途. CN: CN105085433A, 2015-11-25.
[23] 杨春皓, 缪泽鸿, 岳智洲, 梁玉坤, 冯建明, 李佳昕, 贺茜. 一种蒽醌并噻唑化合物、其制备方法及其用途. CN: CN104250246A, 2014-12-31.
[24] 杨春皓, 蒙凌华, 陈艳红, 王祥, 谭村, 李家鹏, 丁健, 陈奕. 吡咯2,1-f1,2,4并三嗪类化合物,其制备方法及用途. CN: CN103450204A, 2013-12-18.
[25] 杨春皓, 缪泽鸿, 丁健, 王猛, 贺金雪, 谭村, 陈奕. 2-芳基苯并呋喃-7-甲酰胺类化合物、其制备方法及用途. CN: CN103242273A, 2013-08-14.
[26] 杨春皓, 缪泽鸿, 丁健, 王猛, 贺金雪, 谭村, 陈奕. 2-芳基苯并呋喃-7-甲酰胺类化合物、其制备方法及用途. CN: CN103242273B, 2015-06-03.
[27] 杨春皓, 江敏, 王祥, 蒙凌华, 丁健. 一类三嗪类化合物、该化合物的制备方法及其用途. CN: CN102887867A, 2013-01-23.
[28] 王猛, 贺茜, 杨春皓, 李晓华, 陈奕, 缪泽鸿. 一类喹啉-8-甲酰胺类化合物、其制备方法及其医药用途. CN: CN102827142A, 2012-12-19.
[29] 王玉勤, 贺茜, 杨春皓, 缪泽鸿, 陈奕, 丁健. 一类苯并咔唑酰胺类化合物、其制备方法和用途. CN: CN102584679A, 2012-07-18.
[30] 王嘉, 蒙凌华, 杨春皓, 王祥, 丁健, 谢毓元. 吡啶并吡咯三嗪化合物、其制备方法和用途. CN: CN102558185A, 2012-07-11.
[31] 江敏, 贺茜, 杨春皓, 谢毓元. 一类莽草酸类化合物及其制备方法和用途. CN: CN101723930A, 2010-06-09.
[32] 陈冬冬, 杨春皓, 严雪铭, 谢毓元. 3-苯基喹啉类化合物、其制备方法和用途. CN: CN101906072A, 2010-12-08.
[33] 陈冬冬, 杨春皓, 严雪铭, 谢毓元. 雌酚酮类化合物及其制备方法和用途. CN: CN101906128A, 2010-12-08.
[34] 贺茜, 杨春皓, 吴茂江, 缪泽鸿, 丁健, 谢毓元. 一类3位取代的1,8－萘酰亚胺类化合物及其合成方法和医药用途. CN: CN101684094A, 2010-03-31.
[35] 吴茂江, 杨春皓, 谢毓元. 5’－((5－甲氧甲氧基－2－苯基吲哚－1－基)亚甲基)－2’－氧代－3’－亚甲基四氢呋喃的制备方法. CN: CN101575331A, 2009-11-11.
[36] 陈五红, 杨春皓, 谢毓元, 沈旭, 王明伟. 选择性雌激素受体亚型调节剂及其合成方法和医药用途. CN: CN101147737A, 2008-03-26.
[37] 吴茂江, 丁健, 陈奕, 林莉萍, 杨春皓, 谢毓元. 4,5－二取代苯基－1,2,3－噻二唑类衍生物,及其制备方法和用途. CN: CN1865252A, 2006-11-22.
[38] 陈五红, 杨春皓, 谢毓元. 3－取代喹啉衍生物及其合成方法. CN: CN101041634A, 2007-09-26.
[39] 陈五红, 贺茜, 杨春皓, 谢毓元. 3－取代的1，2，3，4－四氢喹啉衍生物及其合成方法和用途. CN: CN1817863A, 2006-08-16.
[40] 刘博, 陈五红, 杨春皓, 谢毓元. 3－（2，4，5－三氟－3－甲氧基－苯基）－3氧代－丙酸乙酯的制备方法. CN: CN1789232A, 2006-06-21.
[41] 吉庆刚, 杨春皓, 王明伟, 谢毓元. 一类苯并吡喃4,3－b吲哚化合物、其制备方法和用途. CN: CN1966507A, 2007-05-23.
[42] 丁华胜, 张超, 吴希罕, 杨春皓, 章雄文, 丁健, 谢毓元. 一类α－亚甲基－γ－丁内酯化合物、其制备方法及应用. CN: CN1872851A, 2006-12-06.
[43] 刘博, 杨春皓, 谢毓元, 吴希罕. 一类喹诺酮羧酸化合物及其制备方法和用途. CN: CN1858052A, 2006-11-08.
[44] 刘博, 吴希罕, 杨春皓, 谢毓元. 手性哌嗪取代的喹诺酮羧酸衍生物及其制备方法和用途. CN: CN1778800A, 2006-05-31.
[45] 王军波, 杨春皓, 严雪铭, 吴希罕, 谢毓元. 骨靶向药物、合成方法及用途. CN: CN1660861A, 2005-08-31.
[46] 杨春皓, 吴希罕, 李佳, 王明伟, 谢毓元. 茚酮并吲哚类化合物、制备方法及它的医学用途. CN: CN1566092A, 2005-01-19.
[47] 杨春皓, 李佳, 王明伟. 一类苯并噻吩类化合物、及制备和它的医药用途. CN: CN1548434B, 2010-07-28.

出版信息

发表论文

[1] Yuanyuan Yu, Wenlong Yuan, Jiaqi Yuan, Wenhui Wei, Qian He, Xiaofei Zhang, Shijun He, Chunhao Yang. Synthesis and biological evaluation of pyrazole-fused oleanolic acid derivatives as novel inhibitors of inflammatory and osteoclast differentiation. BIOORGANIC & MEDICINAL CHEMISTRY[J]. 2023, 第 8 作者  通讯作者  80: 117177, http://dx.doi.org/10.1016/j.bmc.2023.117177.
[2] Journal of Medicinal Chemistry. 2023,   通讯作者
[3] Liu, Fangran, Zhuang, Zhen, Qun, Qun, Zhang, Xiaofei, Yang, Chunhao. Ru-Catalyzed Defluorinative Alkylation or Catalyst-Free Hydroalkylation of gem-Difluoroalkenes Enabled by Visible Light. JOURNAL OF ORGANIC CHEMISTRY[J]. 2022, 第 5 作者  通讯作者  87(5): 2730-2739, http://dx.doi.org/10.1021/acs.joc.1c02662.
[4] Yang, Kai, Li, Shunyao, Wang, Tianqi, Yan, Xueming, He, Qian, Ning, Ruonan, Xu, Xing, Yao, Wei, Zhang, Xiaofei, Yang, Chunhao, Jiang, Min, Deng, Lianfu. Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-?B Ligand. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2022, 第 10 作者  通讯作者  65(16): 10992-11009, http://apps.webofknowledge.com/CitedFullRecord.do?product=UA&colName=WOS&SID=5CCFccWmJJRAuMzNPjj&search_mode=CitedFullRecord&isickref=WOS:000841501700001.
[5] Huan, Xiang, Wang, Yanhui, Peng, Xiaofeng, Xie, Shanshan, He, Qian, Zhang, Xiaofei, Lan, Lefu, Yang, Chunhao. Design, synthesis, and biological evaluations of substituted pyrazoles as pyrrolomycin analogues against staphylococcal biofilm. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2022, 第 8 作者  通讯作者  236: http://dx.doi.org/10.1016/j.ejmech.2022.114309.
[6] Zhang, Zhucheng, He, Qian, Zhang, Xiaofei, Yang, Chunhao. Photoredox-catalysed regioselective synthesis of C-4-alkylated pyridines with N-(acyloxy)phthalimides. ORGANIC & BIOMOLECULAR CHEMISTRY[J]. 2022, 第 4 作者  通讯作者  20(9): 1969-1973, http://dx.doi.org/10.1039/d2ob00123c.
[7] Fang, Haotian, Wu, Yingming, Xiao, Qitao, He, Dongbo, Zhou, Tongrui, Liu, Wenzhong, Yang, ChunHao, Xie, Yuli. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S)). BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2022, 第 7 作者72: http://dx.doi.org/10.1016/j.bmcl.2022.128729.
[8] Fang, Haotian, Wu, Yingming, Xiao, Qitao, He, Dongbo, Zhou, Tongrui, Liu, Wenzhong, Yang, ChunHao, Xie, Yuli. Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S)). BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2022, 第 7 作者72: http://dx.doi.org/10.1016/j.bmcl.2022.128729.
[9] 杨春皓. 特效重金属解毒剂的故事. 家庭用药. 2022, 第 1 作者10-11, http://lib.cqvip.com/Qikan/Article/Detail?id=7108237727.
[10] Wang, Jie, Wei, Wenhui, Zhang, Xiaofei, Cao, Shiqi, Hu, Bintao, Ye, Yang, Jiang, Min, Wang, Tianqi, Zuo, Jianping, He, Shijun, Yang, Chunhao. Synthesis and Biological Evaluation of C-17-Amino-Substituted Pyrazole-Fused Betulinic Acid Derivatives as Novel Agents for Osteoarthritis Treatment. JOURNAL OF MEDICINAL CHEMISTRY[J]. 2021, 第 11 作者  通讯作者  64(18): 13676-13692, http://apps.webofknowledge.com/CitedFullRecord.do?product=UA&colName=WOS&SID=5CCFccWmJJRAuMzNPjj&search_mode=CitedFullRecord&isickref=WOS:000701513400032.
[11] Jiaqi Yuan, Xiaofei Zhang, Chunhao Yang. Regioselective Pd-catalyzed α-alkylation of furans using alkyl iodides †. RSC ADVANCES. 2021, 第 3 作者11(23): 13832-13838, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8697702/.
[12] Xiang, HaoYue, Wang, Xiang, Chen, YanHong, Zhang, Xi, Tan, Cun, Wang, Yi, Su, Yi, Gao, ZhiWei, Chen, XiaoYan, Xiong, Bing, Gao, ZhaoBing, Chen, Yi, Ding, Jian, Meng, LingHua, Yang, ChunHao. Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo2,1-f1,2,4triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY[J]. 2021, 第 15 作者209: 10, http://dx.doi.org/10.1016/j.ejmech.2020.112913.
[13] Zhang, Lanfei, Zhang, Xiaofei, Cui, Yongmei, Yang, Chunhao. Direct Approach to 3-Fluoroindoles and 3,3-Difluoroindolines from 2,2-Difluoro-2-phenylethan-1-amines via C-H/N-H Coupling. SYNTHESIS-STUTTGART[J]. 2021, 第 4 作者  通讯作者  53(20): 3815-3826, http://dx.doi.org/10.1055/a-1509-8624.
[14] European Journal of Medicinal Chemistry. 2021,   通讯作者
[15] Wang, Yuxiang, Zhang, Xu, Ma, Qingyang, Hu, Landian, Zhang, Xi, Wang, Yi, Xu, Lan, Yang, Chunhao, Tan, Cun, Kong, Xiangyin, Ding, Jian, Meng, Linghua. Adaptive resistance to PI3K alpha-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells. CELL DEATH & DISEASE[J]. 2021, 第 8 作者12(1): http://dx.doi.org/10.1038/s41419-020-03370-4.
[16] Li, Shunyao, Zhang, Lanfei, He, Qian, Zhang, Xiaofei, Yang, Chunhao. Synthesis of 2-alkyl-chroman-4-ones via cascade alkylation-dechlorination of 3-chlorochromones. ORGANIC & BIOMOLECULAR CHEMISTRY[J]. 2021, 第 5 作者  通讯作者  19(24): 5348-5352, http://dx.doi.org/10.1039/d1ob00463h.
[17] Yuan, Jiaqi, Zhang, Xiaofei, Yang, Chunhao. Regioselective Pd-catalyzed alpha-alkylation of furans using alkyl iodides. RSC ADVANCES[J]. 2021, 第 3 作者  通讯作者  11(23): 13832-13838, http://dx.doi.org/10.1039/d1ra01522b.
[18] Xiang, HaoYue, Chen, JianYang, Huan, XiaJuan, Chen, Yi, Gao, Zhaobing, Ding, Jian, Miao, ZeHong, Yang, ChunHao. Identification of 2-substituted pyrrolo1,2-bpyridazine derivatives as new PARP-1 inhibitors. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2021, 第 8 作者  通讯作者  31: http://dx.doi.org/10.1016/j.bmcl.2020.127710.
[19] Liu, Fangran, Zhang, Xiaofei, Qian, Qun, Yang, Chunhao. A Concise and Efficient Approach to 2,6-Disubstituted 4-Fluoropyrimidines from alpha-CF3 Aryl Ketones. SYNTHESIS-STUTTGART[J]. 2020, 第 4 作者  通讯作者  52(2): 273-280,
[20] Dai, Tianzi, Cui, Chen, Qi, Xueyu, Cheng, Yanshu, He, Qian, Zhang, Xiaofei, Luo, Xiaomin, Yang, Chunhao. Regioselective synthesis of substituted thiazoles via cascade reactions from 3-chlorochromones and thioamides (vol 18, pg 6162, 2020). ORGANIC & BIOMOLECULAR CHEMISTRY. 2020, 第 8 作者  通讯作者  18(47): 9726-9726, http://dx.doi.org/10.1039/d0ob90161j.
[21] Xiang, HaoYue, Chen, YanHong, Wang, Yi, Zhang, Xi, Ding, Jian, Meng, LingHua, Yang, ChunHao. Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo 2,1-f 1,2,4 triazine derivatives. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS[J]. 2020, 第 7 作者  通讯作者  30(12): http://dx.doi.org/10.1016/j.bmcl.2020.127194.
[22] Wang, Yuxiang, Li, Xian, Liu, Xueling, Wang, Bobo, Chen, Yi, Yang, Chunhao, Ding, Jian, Meng, Linghua. Simultaneous inhibition of PI3K alpha and CDK4/6 synergistically suppresses Kras-mutated non-small cell lung cancer. MOLECULAR CANCER RESEARCH. 2020, 第 6 作者18(10): 44-45, https://www.webofscience.com/wos/woscc/full-record/WOS:000576804500063.
[23] Dai, Tianzi, Cui, Chen, Qi, Xueyu, Cheng, Yanshu, He, Qian, Zhang, Xiaofei, Luo, Xiaomin, Yang, Chunhao. Regioselective synthesis of substituted thiazoles via cascade reactions from 3-chlorochromones and thioamides. ORGANIC & BIOMOLECULAR CHEMISTRY[J]. 2020, 第 8 作者  通讯作者  18(31): 6162-6170, https://www.webofscience.com/wos/woscc/full-record/WOS:000558540500020.
[24] Peng, Yingyuan, He, Qian, Zhang, Xiaofei, Yang, Chunhao. Pd-Catalyzed intramolecular C-H activation and C-S formation to synthesize pyrazolo5,1-bbenzothiazoles without an additional oxidant. ORGANIC CHEMISTRY FRONTIERS[J]. 2019, 第 4 作者  通讯作者  6(18): 3234-3237, https://www.webofscience.com/wos/woscc/full-record/WOS:000484960000007.
[25] Peng, Xiaofeng, Zhang, Xiaofei, Li, Shunyao, Lu, Yunfu, Lan, Lefu, Yang, Chunhao. Silver-mediated synthesis of novel 3-CF3/CN/phosphonate-substituted pyrazoles as pyrrolomycin analogues from 3-formylchromones and diazo compounds. ORGANIC CHEMISTRY FRONTIERS[J]. 2019, 第 6 作者  通讯作者  6(11): 1775-1779, https://www.webofscience.com/wos/woscc/full-record/WOS:000469257000004.
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