Medicinal Chemistry in General:

1. Study anti-tumor activities of small molecules that selectively targeting specific proteins, including but not limited to MDM2, MDM4, BRD2~4 and BRDT, BCL2, BFL-1, MCL-1, BCL-xL, TEAD1~4, PD1/PD-L1

2. Modulation of apoptosis pathway, cell cycle pathway, NF-kB2 pathway, and T cell immunity by specific small molecules 

3. Structure-based design and synthesis of inhibitors for kinases, including but not limited to NIK, ASK1, EGFR, COT-1

4. Synthesis of bioactive natural products and their derivatives, evaluation of their antiproliferative activities and potential medical use

Our lab welcomes international applicants pursuing Master and/or Ph.D degrees. 

Only applicants with good training in organic synthesis will be considered.

Nanyang Technological University, Singapore 05/2005-11/2008

Ph.D. in Organic Chemistry

Supervisor: Prof. Teck-Peng Loh 

National University of Singapore, Singapore 08/2003-04/2005

Ph.D. candidate in Organic Chemistry

Transferred in 2005 with Prof. Teck-Peng Loh

Soochow University, Jiangsu Province, P. R. China 09/1999-06/2003

B.S. in Chemistry Education

Thesis Advisor: Prof. Shun-Jun Ji

Professor and Principle Investigator 03/2015-Now

Division of Medicinal Chemistry, Shanghai Institute of Materia Medica, 

Chinese Academy of Science.

Research Investigator 04/2012–03/2015

Division of Hematology/Oncology, Department of Internal Medicine, 

University of Michigan, Ann Arbor, Michigan, USA. 

Supervisor: Prof. Shaomeng Wang        

Postdoctoral Research Fellow 06/2009–03/2012

Division of Hematology/Oncology, Department of Internal Medicine, 

University of Michigan, Ann Arbor, Michigan, USA. 

Supervisor: Prof. Shaomeng Wang    

Project Officer 06/2008–05/2009

Division of Chemistry and Biological Chemistry, 

School of Physical and Mathematical Sciences, 

Nanyang Technological University, Singapore. 

Supervisor: Prof. Teck-Peng Loh 

Advance organic synthesis

Independent Research

1.        Shaozhao Qin, Lijian Feng, Qingyi Zhao, Ziqin Yan, Xilin Lyu, Kaige Li, Baiyang Mu, Yujie Chen, Weiwei Lu, Chao Wang, Yanrui Suo, Jinfeng Yue, Mengqing Cui, Yingjie Li, Yujun Zhao,* Zhiqiang Duan,* Jidong Zhu,* and Xiaojie Lu,* Discovery and Optimization of WDR5 Inhibitors via Cascade 2 Deoxyribonucleic Acid-Encoded Library Selection Approach, Journal of Medicinal Chemistry, 2024, 66, DOI: 10.1021/acs.jmedchem.3c01463.

2.        Jing Cheng, Ziqin Yan, Xinzhi Li, Chen Liu, Linjiang Tong, Xilin Lyu, Bingjie Yang, Zheng Chen,* Yujun Zhao*, Structure-based optimization of indoline-containing compounds as second generation inhibitors of NF-κB-inducing kinase (NIK). Journal of Molecular Structure, 2024, 136755.

3.        Jing Cheng, Ziqin Yan, Kailong Jiang, Chen Liu, Dehua Xu, Xilin Lyu, Xiaobei Hu, Shiyan Zhang, Yubo Zhou,* Jia Li,* Yujun Zhao*, Discovery of JN122, a Spiroindoline-containing Molecule, that Inhibits MDM2/p53 Protein-protein Interaction and Exerts Robust in vivo Antitumor Efficacy. Journal of Medicinal Chemistry, 2023, 66, 16991-17025.

4.        Ziqin Yan, Xilin Lyu, Dongze Lin, Gaoxing Wu, Yang Gong, Xuelian Ren, Jian Xiao, Jianfeng Lou, He Huang, Yi Chen*, Yujun Zhao*, Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines, European Journal of Medicinal Chemistry, 2023, 115381.

5.        Ying Cheng, Xilin Lyu, Chen Liu, Xiancheng Wang, Jing Cheng, Daizhou Zhang,  Xiangjing Meng,* Yujun Zhao*, Synthesis and biological evaluation of sclareolide-indole conjugates and their derivatives. Molecules, 2023, 28, 1737. (IF: 4.92, Year 2022)

6.        Mengnisa Seydimemet, Yixuan Yang, Yuhan Lv, Jiaxiang Liu, Ziqin Yan, Yujun Zhao*, Xuan Wang*, Xiaojie Lu*, Design, construction, and screening of diversified pyrimidine-focused DNA-encoded libraries, ACS Med. Chem. Lett. 2023, 14, 1073−1078.

7.       Shiyan Zhang, Ziqin Yan, Yafang Li, Yang Gong, Xilin Lyu, Jianfeng Lou, Daizhou Zhang, Xiangjing Meng*, Yujun Zhao*, Structure-based discovery of MDM2/4 dual inhibitors that exert antitumor activities against MDM4 -overexpressing cancer cells, Journal of Medicinal Chemistry, 2022, 65, 6207-6230. (IF: 8.03, Year 2022)

8.       Xuexin Feng, Ziqin Yan, Feilong Zhou, Jianfeng Lou, Xilin Lyu, Xuelian Ren, Ziyu Zeng, Chenglong Liu, Shiyan Zhang, Di Zhu, He Huang, Jinming Yang*, Yujun Zhao*, Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells, European Journal of Medicinal Chemistry, 2022, 114327. (IF: 7.08, Year 2022)

9.       Jianfeng Lou, Yuhang Lu, Jing Cheng, Feilong Zhou, Ziqin Yan, Daizhou Zhang, Xiangjing Meng,* Yujun Zhao*, A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities, European Journal of Medicinal Chemistry, 2022, 114684. (IF: 7.08, Year 2022)

10.    Shiyan Zhang, Jianfeng Lou, Yafang Li, Feilong Zhou, Ziqin Yan, Xilin Lyu, Yujun Zhao*, Recent progress and clinical development of inhibitors that block MDM4/p53 protein-protein interactions, Journal of Medicinal Chemistry, 2021, 64, 10621–10640. (IF: 7.44, Year 2021)

11.    Chenglong Liu, Feilong Zhou, Ziqin Yan, Lian Shen, Xichen Zhang, Fenglian He, Xiaojie Lu, Heng Wang, Ker Yu, Yujun Zhao*, Di Zhu*, Discovery of a novel, potent, and selective small-molecule inhibitor of PD-1/PD-L1 interaction with robust in vivo anti-tumor efficacy, British Journal of Pharmacology, 2021, 178, 2651-2670. (IF: 8.73, Year 2021)

12.    Xuan Wang, Jiaxiang Liu, Ziqin Yan, Xiaohong Liu, Sixiu Liu, Yanrui Suo, Weiwei Lu, Jinfeng Yue, Kaixian Chen, Hualiang Jiang, Yujun Zhao*, Mingyue Zheng*, Dongcheng Dai*, Xiaojie Lu*, Diversified strategy for the synthesis of DNA-encoded oxindole libraries, Chemical Science, 2021, 12, 2841-2847. (IF: 9.82, Year 2021)

13.    Jing Cheng, Xuexin Feng, Zhiqiang Li, Feilong Zhou, Jin-Ming Yang, Yujun Zhao*, Pharmacological inhibition of NF-κB-inducing Kinase (NIK) with small molecules for the treatment of human diseases, RSC Medicinal Chemistry, 2021, 12, 552-565.

14.    Xian Zhou, Xuexin Feng, Dachi Wang, Deheng Chen, Gaoxing Wu, Ziqin Yan, Xilin Lyu, Huan Wang, Jin-Ming Yang,* Yujun Zhao*, Synthesis and bioactivity studies of covalent inhibitors derived from (-)-Chaetominine, Journal of Molecular Structure, 2021, 1241, 130694. (IF: 3.19, Year 2021)

15.    Xinzhi Li, Bingchuan Yuan, Min Lu , Yuqin Wang, Na Ding, Chunhong Liu, Ming Gao, Zhicheng Yao, Shiyan Zhang, Yujun Zhao, Liwei Xie, Zheng Chen*, The methyltransferase METTL3 negatively regulates nonalcoholic steatohepatitis (NASH) progression, Nature Communications, 2021, 12, 7213.

16.    Zhiqiang Li, Xinzhi Li, Ming-Bo Su, Li-Xin Gao, Yu-Bo Zhou, Bingchuan Yuan, Xilin Lyu, Ziqin Yan, Chujiao Hu, Hao Zhang, Cheng Luo, Zheng Chen*, Jia Li*, Yujun Zhao*, Discovery of a potent and selective NF-κB-inducing kinase (NIK) inhibitor that has anti-inflammatory effects in vitro and in vivo, Journal of Medicinal Chemistry, 2020, 63, 4388-4407. (IF: 7.44, Year 2021)

17.    Shiyan Zhang, Chaoying Huang, Xilin Lyu, Peipei Wang, Yi Zang, Zengtao Wang, Huan Wang, Jia Li*, Yujun Zhao*, Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal -regulating kinase 1 (ASK1), European Journal of Medicinal Chemistry, 2020, 195, 112277. (IF: 6.51, Year 2021)

18.    Xinzhi Li, Yongsen Wu, Yue Song, Na Ding, Min Lu, Linna Jia, Yujun Zhao, Ming Liu, Zheng Chen*, Activation of NF-kB-inducing kinase in islet β-cells causes β-cell failure and diabetes, Molecular Therapy, 2020, 2430-2441. (IF: 11.45, Year 2021)

19.    Deheng Chen, Tian Lu, Ziqin Yan, Wenchao Lu, Feilong Zhou, Xilin Lyu, Biling Xu, Hualiang Jiang, Kaixian Chen, Cheng Luo*, and Yujun Zhao*, Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins, European Journal of Medicinal Chemistry, 2019, 182, 111633. (IF: 6.51, Year 2021)

20.    Erbao Zhao, Feilong Zhou, and Yujun Zhao*, Lewis Acids Promoted 3+2 Cycloaddition of Oxaziridines and Cyclic Allylic Alcohols through Carbonyl Imine Intermediates, Journal of Organic Chemistry, 2019, 84 (7), 4282–4293. (IF: 4.35, Year 2021 )

21.    Deheng Chen, Dexiang Guo, Ziqin Yan, Yujun Zhao*, Allenamide as a bioisostere of acrylamide in design and synthesis of targeted covalent inhibitors Med. Chem. Commun. 2018, 9, 244-253. (IF: 2.80, Year 2020)

22.    Feilong Zhou, Erbao Zhao, Ziqin Yan, Deheng Chen, Yujun Zhao*, Synthesis of 3,4-diarylsubstituted hexahydro-1H-indoles, Tetrahedron Letters, 2018, 59, 1871-1874. (IF: 2.41, Year 2021)

23.    Xiaomeng Ren, Xinzhi Li, Linna Jia, Deheng Chen, Hai Hou, Liangyou Rui, Yujun Zhao*, Zheng Chen*, A small-molecule inhibitor of NF-kB-inducing kinase (NIK) protects liver from toxin-induced inflammation, oxidative stress, and injury, FASEB Journal. 2017, 2, 711-718. (IF: 5.19, Year 2021) 

Patents Based on Independent Research

1.        赵玉军，程靖，严子琴，吕细林，张世言，周飞龙，具有取代苯基螺[吲哚啉-3,3'-吡咯烷]结构的小分子化合物，PCT patent application number： WO202211255892.0；Application date：2022-10-14；

2.        赵玉军，朱棣，周飞龙，严子琴，刘成龙，曾子余，程颖，具有苄氧基芳基醚结构的化合物及其制备方法和用途，PCT patent application number：WO202210220889.9；Application date：2022-03-09；

3.        赵玉军，张世言，严子琴，吕细林，周飞龙，具有4-(取代氨甲基)-5-新戊基-N-取代基吡咯烷-2-甲酰胺结构的化合物，PCT patent application number: WO202111571938.5；Application date：2021-12-21；

4.        赵玉军，张世言，严子琴，吕细林，程靖，周飞龙，巩洋，具有取代苯基螺[吲哚啉-3,3’-吡咯烷]结构的小分子化合物，PCT patent application number: WO2022218379；Application date：2021-04-15；

5.        赵玉军，李志强，严子琴，李亚芳，吕细林，周飞龙，苯并含氮五元杂环化合物及其合成和应用，中国专利申请号：202110476362.8；Application date：2021-04-30；

6.        赵玉军，朱棣，周飞龙， 严子琴，刘成龙，张希晨， 一种具有苄氧基芳环结构的化合物,其制备方法和用途, PCT patent application number: WO2020244518, Application date: 2020-06-02; China Patent Number: ZL202010491651.0，Application data: 2020-06-03

7.        赵玉军，王欢，陈德恒，周飞龙， 严子琴，吕细林，具有2H-吲唑结果的小分子化合物及其合成和应用，China Patent Number: ZL202010135402.8, Application date: 2020.03.02

8.        赵玉军、李佳、王增涛、张世言、臧奕、王培培、孙丹丹、张含烟, 2-吡啶取代脲结构小分子化合物及其合成和应用，中国专利申请号: 201910716810.X, Application date: 2019-08-05

9.        赵玉军、陈德恒、郭德祥、严子琴、周飞龙、耿美玉、丁健、沈爱军、刘红椿、张敏敏，一种BRD4 抑制剂及其制备和应用, China Patent Number: ZL201880024931.1, Publication date: 2018-04-13; PCT patent application number: WO2018/188660, Application date: 2018-10-18;

10.    赵玉军，李志强，严子琴，李佳，周宇波，苏明波，陈政，一种具有2-氨基嘧啶结构的化合物，其制备方法和用途，China Patent Application Number: 201811381899.0, Application date: 2018-11-20；

11.    赵玉军、郭德祥、严子琴，含有共轭联烯酰胺结构的化合物、其制备方法、药物组合物和用途, China Patent Number: ZL201711105956.8, Application data: 2017-11-10;

12.    赵玉军、陈德恒、严子琴，郭德祥，含有共轭联烯结构的化合物、其药物组合物和用途, China Patent Number: ZL201710639753.0, Application date: 2017-07-31.

Co-author Patents:

1.        Shaomeng Wang*, Yujun Zhao, Bing Zhou, Angelo Aguilar, Liu Liu, Longchuan Bai, Donna McEachern, Duxin Sun, Bo Wen, Ruijuan Luo, and Ting Zhao, 9H-Pyrimido[4,5-B]indoles and Related Analogs as BET Bromodomain Inhibitors, 2015.2, PCT Patent Publication No.: WO2015131005 A1; US Patent No.: US9580430B2 (2017-02-28), US10253044B2 (2019-04-09).

2.        Shaomeng Wang*, Xu Ran, Yujun Zhao, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachern, Jeanne Stuckey, Jennifer Lynn Meagher, Duxin Sun, Xiaoqin Li, Bing Zhou, Hacer Karatas, Ruijuan Luo, Arul Chinnaiyan, Irfan A. Asangani, BET Bromodomain Inhibitors and therapeutic Methods Using the same, 2014.10.9, PCT Patent Publication No.: WO2014164596 A1; China Patent No.: CN105377851B (2018-07-20); US Patent No.: US9675697B2 (2017-06-13), US10391175B2 (2019-08-27).

3.        Shaomeng Wang*, Yujun Zhao, Wei Sun, Sanjeev Kumar, Lance Leopold, Laurent Debussche, Cedric Barriere, Jeanchristophe Carry, Kwame Amaning, Spiro-Oxindole MDM2 Antagonists, 2012.5.18, PCT Patent Publication No.: WO 2012/065022 A2; US Patent No.: CN103298818B (2016.6.29); US Patent No.: US9302120B2 (2016-04-05)

4.        Shaomeng Wang*, Shanghai Yu, Wei Sun, Sanjeev Kumar Shangary, Duxin  Sun, Peng Zou, Donna McEachern, Yujun Zhao, Spiro-Oxindole MDM2 Antagonists, 2011.5.19, PCT Patent Publication No.: WO 2011060049; China Patent No.: CN102712650 B (2015-05-20); US Patent No.: US8518984 B2 (2013.8.27); US8877796B2 (2014-11-04).

5.        Shaomeng Wang*, Jianyong Chen, Yujun Zhao, Cindy Gomez, Longchuan Bai, Zeneta Nikolovska-Coleska, STAT3 Ligands and Therapeutic Uses Thereof, 2010.7.8, PCT Patent Publication No.: WO 2010077589; US Patent Publication No.: US 2011/0319362; China Patent Publication No.: CN 200980156486; European Patent Publication No.: EP2373658 A4

6.        Teck-Peng Loh*, Yujun Zhao, Cyclization Process of Forming a Multiple Ring Compound. 2007.2, PCT Patent Publication No.: WO 2007097719; US Patent No.: US8227645 B2 (2012.1.4);

Inhibitors of Kinases and Protein-protein interactions 

Small molecules induce cell apoptosis

Small molecules with anti-tumor activtiy

Synthesis and evaluation of bioactive natural products

DMPK-tox study and drug development

已指导学生

陈德恒  博士研究生  100701-药物化学  

吴高星  硕士研究生  078001-药物化学  

张希晨  硕士研究生  078001-药物化学  

李志强  博士研究生  100701-药物化学  

张世言  博士研究生  100701-药物化学  

现指导学生

程靖  博士研究生  100701-药物化学  

路宇航  博士研究生  100701-药物化学  

周泽惠  博士研究生  100701-药物化学  

王先城  硕士研究生  078001-药物化学  

楼剑锋  博士研究生  100701-药物化学  

吴非飞  博士研究生  100701-药物化学