Shanghai Institute of Material Medical Chinese Academy of Sciences

Biography

Dr. YANG Chunhao, Principal investigator of Shanghai Institute of Materia Medica, Chinese Academy of Sciences. Yang received his BSc in chemistry from Suzhou University in 1992, and his MSc from East China Normal University in 1995. After he obtained his PhD in organic chemistry at Shanghai Institute of Materia Medica in 2003, he joined Prof. XIE Yuyuan’s group in the same institute and was elected as a group leader in 2010. His current research interest focuses on the discovery of novel anti-cancer agents, anti-osteoporosis/osteoarthritis agents, and the development of bioactive heterocycle-oriented methodology. He published more than 90 peer-reviewed articles and filed twenty patents including 5 PCT patents.

Education

09/1988-06/1992, Suzhou University (B.S. in chemistry)

09/1992-06/1995, East China Normal University (M.S. in organic chemistry)

08/2000-07/2003, Shanghai Institute of Materia Medica (Ph.D. in organic chemistry)

Work Experience

08/1995-07/2000, Lecturer, Chemical Education Group, Medical School of Nantong University.

08/2008-01/2009, Visiting Scholar, Department of Chemistry, Georgia State University.

08/2003-present, Assiatant/Associate/Full Professor, Department of Medicinal Chemistry, Shanghai Institute of Materia Medica.

Research Directions

1.Discovery of novel anti-cancer agents.

2.Discovery of novel anti-osteoporosis/osteoarthritis agents.

3.Developing rapid synthetic methodologies for novel heterocycles with potential bioactivities.

Grants & Research Projects

National Science & Technology Major Project “Key New Drug Creation and Manufacturing Program” , Clinical Trial of PARP inhibitor mefuparib hydrochloride, Project Leader, 2019.1-2020.12

Achievements

1. More than 70 libraries of heterocyclic compounds were constructed using effective one-pot cascade reactions or metal-catalyzed C-H activation. Based on these libraries, many compounds with novel bioactive mechanism were found, such as PI3K/Tubulin dual inhibitor S9, DNA TopⅡ/Tubulin dual inhibitor YCH337.

2. Dr. YANG led the discovery of two anti-cancer drug candidates for targeted therapy in clinical trials: PARP1/2 inhibitor Mefuparib hydrochloride is in Phase Ⅰ in China. The phase Ⅰa of PI3Kα inhibitor CYH33 has completed in China and its IND in US was approved in 2020. Several drug candidates are in preclinical stage.

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Social Titles

1.Member of Chinese Pharmaceutical Association

2.Member of Division of Tumor Pharmacology, Chinese Pharmacological Society

3.Member of American Association of Cancer Research

4.Member of International Society of Heterocyclic Chemistry

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Awards & Honors

1.11/2009, Shanghai Science & Technology Progress Award

2.10/2013, MEIJI Life Science Award

3.08/2015, Zhu-Li Yuehua Award for Prominent Teacher

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Pubilcations

Full Publication List

Selected Publications

1.Hao-Yue Xiang, Xiang Wang, Yan-Hong Chen, Xi Zhang, Cun Tan, Yi Wang, Yi Su, Zhi-Wei Gao, Xiao-Yan Chen, Bing Xiong, Zhao-Bing Gao, Yi Chen, Jian Ding,* Ling-Hua Meng,* and Chun-Hao Yang.*Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo [2,1-f][1,2,4]triazin-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. Eur. J. Med. Chem. 2021, 209, 112913.

https://doi.org/10.1016/j.ejmech.2020.112913

2.Min Jiang, Lei Peng, Kai Yang, Tianqi Wang, Xueming Yan, Tao Jiang, Jianrong Xu, Jin Qi, Hanbing Zhou, Niandong Qian, Qi Zhou, Bo Chen, Xing Xu*, Lianfu Deng*, Chunhao Yang* Development of Small Molecules Targeting Receptor Activator of Nuclear Factor-κB Ligand (RANKL) - Receptor Activator of Nuclear Factor-κB (RANK) Protein-Protein Interaction by Structure-Based Virtual Screening and Hit Optimization. J. Med. Chem., 2019, 62, 5370-5381.

DOI: 10.1021/acs.jmedchem.8b02027

3.Xiaofeng Peng, Xiaofei Zhang, Shunyao Li, Yunfu Lu, Lefu Lan * and Chunhao Yang.* Silver-mediated Synthesis of Novel 3-CF3/CN/Phosphonate-substituted Pyrazoles as Pyrrolomycin Analogues from 3-Formylchromones and Diazo Compounds. Org. Chem. Front. 2019, 6, 1775 – 1779.

DOI: 10.1039/C9QO00324J.

4.Xuxing Chen, Xiajuan Huan, Qiufeng Liu,YuqinWang, Qian He, Cun Tan, Yi Chen, Jian Ding, YechunXu,* Zehong Miao,* and ChunhaoYang*. Design and Synthesis of 2-(4,5,6,7-Tetrahydrothienopyridin-2-yl)-benzoimidazole Carboxamides as Novel Orally Efficacious Poly(ADP-ribose)polymerase (PARP) Inhibitors. Eur. J. Med. Chem. 2018, 145, 389-403.

DOI: 10.1016/j.ejmech.2018.01.018

5.Jin-Xue He, Meng Wang, Xia-Juan Huan, Chuan-Huizi Chen, Shan-Shan Song, Ying-Qing Wang, Xue-Mei Liao, Cun Tan, Qian He, Lin-Jiang Tong, Yu-Ting Wang, Xiao-Hua Li, Yi Su, Yan-Yan Shen, Yi-Ming Sun, Xin-Ying Yang, Yi Chen, Zhi-Wei Gao, Xiao-Yan Chen, Bing Xiong, Xiu-Lian Lu, Jian Ding, Chun-Hao Yang,* Ze-Hong Miao.* Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution. Oncotarget. 2017 ;8(3):4156-4168.

DOI: 10.18632/oncotarget.13749

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