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Biography

Prof. Yang received his B.S. in chemistry (1987) and M.S. in organic chemistry (1990) from Sichuan University, and Ph.D. (1996) from Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, under the supervision of Prof. Ruyun Ji. Upon completion of his postdoctoral research in the same group, he joined the SIMM as faculty in 1998. He is now a professor of medicinal chemistry and Principal Investigator at SIMM and Zhongshan Institute for Drug Discovery (ZIDD).

Research Directions

Prof. Yang's research interests focus on new drug discovery and development, spanning anti-infectives, anticoagulants, anticancer drugs and central nervous system drugs.

Achievements

Prof. Yang has been dedicated to new drug discovery and development for over twenty years and has accumulated a wealth of knowledge and experience in the field antibiotics, anticancer drugs and anticoagulants. His endeavors in the field have brought many accomplishments, including two “class 1.1 new drug” certificates. A representative achievement in Yang’s Lab is the successful development of Antofloxacin Hydrochloride, an innovative fluoroquinolone antibiotic. With superior safety, efficacy and pharmacokinetic (PK) profiles over other antibiotics, Antofloxacin was approved by the China Prof. Yang has been dedicated to new drug discovery and development for over twenty years and has accumulated a wealth of knowledge and experience in the field antibiotics, anticancer drugs and anticoagulants. His endeavors in the field have brought many accomplishments, including two “class 1.1 new drug” certificates. A representative achievement in Yang’s Lab is the successful development of Antofloxacin Hydrochloride, an innovative fluoroquinolone antibiotic. With superior safety, efficacy and pharmacokinetic (PK) profiles over other antibiotics, Antofloxacin was approved by the China Science and Technology Award for Technical Invention (ranking first) in 2015, the China Pharmaceutical Development Award (Innovative Drug Award), and Shanghai Advanced Worker (Model Worker).

Publications

1. Zhengyu Lu, Yangzhi Cao, Dan Zhang, Xin Meng, Bin Guo*, Deyu Kong*,Yushe Yang*. Discovery of Thieno[2,3-e]indazole Derivatives as Novel Oral Selective Estrogen Receptor Degraders with Highly Improved Antitumor Effect and Favorable Druggability.J. Med. Chem.2022,65(7), 5724?5750.

2. Huijun Ma#, Anran Qian#, Yazhou Zheng, Xin Meng, Ting Wang, Yinyong Zhang, Lulu Sun, Feng Zou, Bomei Zhao, Shuhua Zhang, Dan Zhang*, andYushe Yang*. Design, Synthesis, and Structure–Activity Relationship Studies of Bisamide Derivatives of Amphotericin B with Potent Efficacy and Low Toxicity.J. Med. Chem.2022,65(13), 8897?8913.

3. Ao Wang, Xianggang Luo, Yawan Wang, Xin Meng, Zhengyu Lu, andYusheYang*. Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.J. Med. Chem.2022,65(18), 12460?12481.

4. Qidi Kong, Wei Pan, Heng Xu, Yaru Xue, Bin Guo, Xin Meng, Cheng Luo, Ting Wang, Shuhua Zhang, andYusheYang*. Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens.J. Med. Chem.2021,64(12), 8644?8665. Chenghui Shi#, Yinyong Zhang#, Ting Wang, Wenchao Lu, Shuhua Zhang, Bin Guo, Qian Chen, Cheng Luo, Xianli Zhou*, andYusheYang*, Design, Synthesis, and Biological Evaluation of

5. Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria.J. Med. Chem.2019, 62(6),2950?2973.

6. Deyu Kong, Tao Xue, Bin Guo, Jianjun Cheng, Shunyin Liu, Jianhai Wei, Zhengyu Lu, Haoran Liu, Guoqing Gong, Tian Lan, Wenhao Hu*, andYusheYang*，Optimization of P2Y12 Antagonist Ethyl 6?(4-((Benzylsulfonyl) carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties.J. Med. Chem.2019,62(6),3088?3106.

7. Liang Tan, Yunliang Tao, Ting Wang, Feng Zou, Shuhua Zhang, Qun huan Kou, Ao Niu, Qian Chen, Wenjing Chu,Xiaoyan Chen, Haidong Wang*, andYusheYang*. Discovery of Novel Pyridone-Conjugated Monosulfactams as Potent and Broad-Spectrum Antibiotics for Multidrug-Resistant Gram-Negative Infections.J. Med. Chem. 2017,60(7), 2669–2684.

8. Tao Xue, Shi Ding, Bin Guo*, Yuren Zhou, Peng Sun, Heyao Wang, Wenjing Chu, Guoqing Gong, Yinye Wang, Xiaoyan Chen, andYusheYang*. Design, Synthesis, and Structure-Activity and Structure-Pharmacokinetic Relationship Studies of Novel [6,6,5] Tricyclic Fused Oxazolidinones Leading to the Discovery of a Potent, Selective, and Orally Bioavailable FXa Inhibitor.J.Med.Chem. 2014,57(18), 7770?7791.

9. Chenyu Ling, Liqiang Fu, Suo Gao, Wenjing Chu, Hui Wang, Yanqin Huang, Xiaoyan Chen, andYusheYang*. Design, Synthesis, and Structure-Activity Relationship Studies of Novel Thioether Pleuromutilin Derivatives as Potent Antibacterial Agents.J. Med. Chem.2014,57(11),4772?4795.

10.Xufeng Cao#, Zhaoshuan Sun#, Yongbing Cao, Ruilian Wang, Wenjing Chu, Wenhao Hu*,YusheYang,* Design, Synthesis, and Structure–Activity Relationship Studies of Novel Fused-Heterocycle- 10.Linked Triazoles with High Activity and Water Solubility. J. Med. Chem. 2014, 57(9), 3687?3760.

11.Bin Guo, Houxing Fan, Qisheng Xin, Wenjing Chu, Hui Wang, Yanqin Huang, Xiaoyan Chen, and Yushe Yang*.Solubility-Driven Optimization of (Pyridin-3-yl) Benzoxazinyl-oxazolidinones Leading to a Promising Antibacterial Agent. J. Med. Chem. 2013, 56(6), 2642?2650.

12.Qisheng Xin#, Houxing Fan#, Bin Guo, Huili He, Suo Gao, Hui Wang, Yanqin Huang, Weiliang Zhu, Yushe Yang*. Design, Synthesis, and Structure–Activity Relationship Studies of Highly Potent Novel Benzoxazinyl-Oxazolidinone Antibacterial Agents. J. Med. Chem. 2011, 54(21), 7493?7502.