LAI, YISHENG

Release date:2016-06-06  Release:


LAI, YISHENG

Professor of Medicinal Chemistry

Institute of Pharmaceutical Sciences

Phone: 86-25-83271015

Email: yslai@cpu.edu.cn

Research Summary

Dr. LAI’s research interest focuses on the design, synthesis and biological evaluation of small molecular agents targeting crucial proteins in human diseases, including cancer and inflammatory disorders. He has discovered some lead compounds with novel structure for important drug targets, among which several candidates are currently undergoing preclinical studies. So far, he has published more than 100 academic papers in the field of medicinal chemistry, organic chemistry and pharmacology, and has applied 29 patents and obtained 10 patent certifications.

Education

2004   Ph.D., Medicinal Chemistry, China Pharmaceutical University

1991   M.S., Physical Chemistry, Chongqing University

1985   B.S., Chemistry, Guangxi Normal University for Nationalities

Academic Experience

2011-present  Professor of Medicinal Chemistry, China Pharmaceutical University

2004-2011  Associate Professor of Medicinal Chemistry, China Pharmaceutical University

1991-2001  Associate Professor of Medicinal Chemistry, Guangxi University of Chinese Medicine

Awards and Honors

2011 Six talent peaks project of Jiangsu Province

Representative Publications

  1. Yong Ai, Bin Zhu, Caiping Ren*, Fenghua Kang, Jinlong Li, Zhangjian Huang*, Yisheng Lai, Sixun Peng, Ke Ding, Jide Tian, Yihua Zhang*. Discovery of new monocarbonyl ligustrazine-curcumin hybrids for intervention of drug-sensitive and drug-resistant lung cancer. J Med Chem, 2016, 59(6): 1747-1760.

  2. Zilei Xia, Jiadong Hu, Zhigao Shen, Xiaolong Wan, Qizheng Yao, Yisheng Lai, Jin-Ming Gao, Weiqing Xie*. Enantioselective bromo-oxycyclization of silanol. Org Lett, 2016, 18(1): 80-83.

  3. Zhigao Shen,Xixian Pan, Yisheng Lai, Jiadong Hu, Xiaolong Wan, Xiaoge Li, Hui Zhang, Weiqing Xie*. Chiral ion-pair organocatalyst promotes highly enantioselective 3-exo iodo-cycloetherification of allyl alcohols. Chem Sci, 2015, 6(12): 6986-6990.

  4. Xiangyang Feng, Guangde Jiang, Zilei Xia, Jiadong Hu, Xiaolong Wan, Jin-Ming Gao, Yisheng Lai*, Weiqing Xie*. Total synthesis of (−)-conolutinine. Org Lett, 2015, 17(18): 4428-4431.

  5. Jianhu Xiao, Shengping Zhang, Minghao Luo, Yi Zou, Yihua Zhang, Yisheng Lai*. Effective virtual screening strategy focusing on the identification of novel Bruton's tyrosine kinase inhibitors. J Mol Graph Model, 2015, 60: 142-154.

  6. Zhigao Shen, Zilei Xia, Huijun Zhao, Jiadong Hu, Xiaolong Wan, Yisheng Lai*, Chen Zhu*, Weiqing Xie*. Synthesis of naked amino-pyrroloindoline via direct aminocyclization of tryptamine. Org Biomol Chem, 2015, 13(19): 5381-5384.

  7. Yong Ai, Yang Hu, Fenghua Kang, Yisheng Lai, Yanju Jia, Zhangjian Huang*, Sixun Peng, Hui Ji*, Jide Tian, Yihua Zhang*. Synthesis and biological evaluation of novel olean-28,13β-lactams as potential antiprostate cancer agents. J Med Chem, 2015, 58(11): 4506-4520.

  8. Yong Ai, Fenghua Kang, Zhangjian Huang*, Xiaowen Xue, Yisheng Lai, Sixun Peng, Jide Tian, Yihua Zhang*. Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. J Med Chem, 2015, 58(5): 2452-2464.

  9. Junjie Fu, Yu Zou, Zhangjian Huang*, Chang Yan, Qimeng Zhou, Huibin Zhang*, Yisheng Lai, Sixun Peng, Yihua Zhang*. Identification of nitric oxide-releasing derivatives of oleanolic acid as potential anti-colon cancer agents. RSC Adv, 2015, 5: 19445-19454.

  10. Shengping Zhang, Jiani Tan, Zhonghui Lai, Ying Li, Junxia Pang, Jianhu Xiao, Zhangjian Huang, Yihua Zhang, Hui Ji*, and Yisheng Lai*. Effective virtual screening strategy toward covalent ligands: identification of novel NEDD8-activating enzyme inhibitors.J Chem Inf Model, 2014,54(6): 1785-1797.

  11. Huan Liu, Guangde Jiang, Xixian Pan, Xiaolong Wan, Yisheng Lai*, Dawei Ma*, Weiqing Xie*. Highly asymmetric bromocyclization of tryptophol: unexpected accelerating effect of DABCO-derived bromine complex. Org Lett, 2014, 16(7): 1908-1911.

  12. Chun Han, Ledong Wan, Hongbin Ji, Ke Ding, Zhangjian Huang*, Yisheng Lai*, Sixun Peng, Yihua Zhang*. Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors. Eur J Med Chem, 2014, 77: 75-83.

  13. Weiqing Xie*, Guangde Jiang, Huan Liu, Jiadong Hu, Xixian Pan, Hui Zhang, Yisheng Lai*, Dawei Ma*. Highly enantioselective bromocyclization of tryptamine and its application on synthesis of (-)-chimonanthine. Angew Chem Int Ed, 2013, 52(49): 12924-12927.

  14. Ran You, Wenyan Long, Zhonghui Lai, Lei Sha, Kai Wu, Xing Yu, Yisheng Lai*, Hui Ji*, Zhangjian Huang, and Yihua Zhang. Discovery of a potential anti-Inflammatory agent: 3-oxo-29-noroleana-1,9(11),12-trien-2,20-dicarbonitrile. J Med Chem, 2013,56(5): 1984-1995.

  15. Ye Zhang, Hui Xing, Weiqing Xie*, Xiaolong Wan, Yisheng Lai*, Dawei Ma*. Asymmetric, regioselective bromohydroxylation of 2-aryl-2-propen-1-ols catalyzed by quinine-derived catalysts. Adv Synth Catal, 2013, 355(1): 68-72.

  16. Jiani Tan, Zhonghui Lai, Ling Liu, Wenyan Long, Tong Chen, Jun Zha, Linna Wang, Meiyu Chen, HuiJi*, Yisheng Lai*. ONTD induces apoptosis of human hepatoma Bel-7402 cells via a MAPK-dependent mitochondrial pathway and the depletion of intracellular glutathione. Int J Biochem Cell Biol, 2013,45(11): 2632-2642.

  17. Junjie Fu, Ling Liu, Zhangjian Huang, Yisheng Lai, Hui Ji*, Sixun Peng, Jide Tian, Yihua Zhang*. Hybrid molecule from O2-(2,4-dinitrophenyl)diazeniumdiolate and oleanolic acid: a glutathione S-transferase π-activated nitric oxide prodrug with selective anti-human hepatocellular carcinoma activity and improved stability. J Med Chem,2013, 56(11): 4641-4655.

  18. Xiaoli Wang, Linna Wang, Tingting Li , Zhangjian Huang, Yisheng Lai, Hui Ji*, Xiaolong Wan, Jinyi Xu, Jide Tian, Yihua Zhang*. Novel hybrids of optically active ring-opened 3-n-butylphthalide derivative and isosorbide as potential anti-ischemic stroke agents. J Med Chem, 2013, 56(7): 3078-3089.

  19. Chun Han, Zhangjian Huang, Chao Zheng, Ledong Wan, Yisheng Lai, Sixun Peng, Ke Ding*, Hongbin Ji*, Yihua Zhang*. Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors. Eur J Med Chem, 2013, 66(1): 82-90.

  20. Li Chen, Hui Ji*, Yisheng Lai*. ZLJ-6, a Novel COX/5-LOX Inhibitor, ameliorates atherosclerosis by reducing macrophage infiltration in ApoE-/- mice. Lat Am J Pharm, 2013, 32(3): 418-424.

  21. Lihong Shen*, Hongyu Li, Shuxian Li, Huimin Bi, Bofeng Xue, Yisheng Lai, Lijie Liu. Synthesis and biological evaluation of nitrate derivatives of thiocolchicine as potential anticancer drugs. Lat Am J Pharm, 2013, 32(2): 220-224.

  22. Feng Cao, Jinghao Jia, Zhi Yin, Yahan Gao, Lei Sha, Yisheng Lai*, Qineng Ping*, Yihua Zhang. Ethylene glycol-linked amino acid diesterprodrugs of oleanolic acid for PepT1-mediated transport: synthesis, intestinal permeability and pharmacokinetics. Mol Pharmaceut,2012, 9(8): 2127-2135.

  23. Hui Xing, Ye Zhang, Yisheng Lai*, Yongwen Jiang, Dawei Ma*. Synthesis of symmetrical and unsymmetrical N,N'-diaryl guanidines via copper/N-methylglycine- catalyzed arylation of guanidine nitrate.J Org Chem, 2012, 77(12): 5449-5453.

  24. Jing Wu, Jingjing Ling, Xuliang Wang, Tingting Li, Jingchao Liu, Yisheng Lai, HuiJi*, Sixun Peng, Jide Tian, Yihua Zhang*. Discovery of a ptential anti-ischemic stroke agent 3-pentylbenzo[c]thiophen-1(3H)-one. J Med Chem, 2012, 55(16): 7173-7181.

  25. Xiaoli Wang, Qian Zhao, Xuliang Wang, Tingting Li, Yisheng Lai, Sixun Peng, Hui Ji*, Jinyi Xu*, Yihua Zhang*. Studies on the enantiomers of ZJM-289: synthesis and biological evaluation of antiplatelet, antithrombotic and neuroprotective activities. Org Biomol Chem, 2012, 10(45): 9030-9040.

  26. Zhangjian Huang, Junjie Fu, Ling Liu, Yijun Sun, Yisheng Lai, Hui Ji*, Edward E. Knaus, Jide Tian, Yihua Zhang*. Glycosylated diazeniumdiolate-based oleanolic acid derivatives: synthesis, in vitro and in vivo biological evaluation as anti-human hepatocellular carcinoma agents.Org Biomol Chem, 2012, 10(19): 3882-3891.

  27. Xiaoke Gu, Zhiguang Ren, Xiaobo Tang, Hui Peng*, Qing Zhao, Yisheng Lai, Sixun Peng, Yihua Zhang*. Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors. Euro J Med Chem,2012, 51: 137-144.

  28. Xiaoke Gu, Zhiguang Ren, Xiaobo Tang, Hui Peng*, Yuanfang Ma, Yisheng Lai, Sixun Peng, Yihua Zhang*. Synthesis and biological evaluation of bifendate-chalcone hybrids as a new class of potential P-glycoprotein inhibitors. Bioorg Med Chem, 2012, 20(8): 2540-2548.

  29. Xiaobo Tang, Xiaoke Gu, Zhiguang Ren, Yuanfang Ma, Yisheng Lai, Hui Peng*, Sixun Peng, Yihua Zhang*. Synthesis and evaluation of substituted dibenzo[c,e]azepine-5- ones as P-gly-coprotein-mediated multidrug resistance reversal agents. Bioorg Med Chem Lett, 2012, 22(8): 2675-2680.

  30. Xiaobo Tang, Xiaoke Gu, Hua Ai, Guangji Wang, Hui Peng*, Yisheng Lai, Yihua Zhang*. Synthesis and evaluation of nitric oxide-releasing DDB derivatives as potential Pgp-mediated MDR reversal agents in MCF-7/Adr cells. Bioorg Med Chem Lett,2012, 22(2): 801-805.

  31. Lingli Zhang, Ning Li, Yisheng Lai, Yihua Zhang, Xijing Chen*, Li Chen, Hui Ji, Cuiyun Li. Pharmacokinetic, distribution, metabolism, and excretion of (Z)-2-amino-1, 5-dihydro-1-methyl-5-[4-(mesyl)benzylidene]-4H-imidazol-4-one mesilate (ZLJ-601) in Sprague-Dawley rats. Pharmacology, 2012, 89(3-4): 192-200.

  32. Yuan Gao, Li Li, Jianjun Zhang*, Feng Su, Zhenhua Gong, Yisheng Lai, Yihua Zhang. Physicochemical characterization and an injection formulation study of water insoluble ZCVI4-2, a novel NO-donor anticancer compound. Arch Pharm Res, 2012, 35(7): 1177-1186.

  33. Xinye Yang, Hui Xing, Ye Zhang, Yisheng Lai, Yihua Zhang*, Yongwen Jiang, Dawei Ma*. CuI/8-hydroxyquinalidine promoted N-arylation of indole and azoles. Chin J Chem, 2012, 30(4): 875-880.

  34. Li Chen, Qian Zhao, Xuliang Wang, Ran You, Yihua Zhang, Hui Ji*, Yisheng Lai*. ZLJ-6, a novel COX/5-LOX inhibitor, attenuates TNF-α-induced endothelial E-selectin, ICAM-1 and VCAM-1 expression and monocyte-endothelial interactions via a COX/5-LOX-independent mechanism. Vasc Pharmacol, 2011, 55(5-6): 135-142.

  35. Li Chen, Liwen Li, Lin Ma, Yihua Zhang, Hui Ji*, Yisheng Lai*. Antiplatelet and antithrombotic effects of ZLJ-6, an inhibitor of cyclooxygenase and 5-lipoxygenase. Lat Am J Pharm, 2011, 30(8): 1506-1511.

  36. Ye Ding, Zhangjian Huang, Jian Yin, Yisheng Lai, Shibo Zhang, Zhiguo Zhang, Lei Fang, Sixun Peng, Yihua Zhang*. DDQ-promoted dehydrogenation from natural rigid polycyclic acids or flexible alkyl acids to generate lactones by a radical ion mechanism. Chem Commun,2011, 47(33): 9495-9497.

  37. Yong Ling, Xiaolei Ye, Zhenzhen Zhang, Yihua Zhang*, Yisheng Lai, Hui Ji*, Sixun Peng, Jide Tian. Novel nitric oxide-releasing derivatives of farnesylthiosalicylic acid: synthesis and evaluation of antihepatocellular carcinoma activity. J Med Chem, 2011,54(9): 3251-3259.

  38. Xuliang Wang, Yang Li, Qian Zhao, Zhenli Min, Chao Zhang, Yisheng Lai, Hui Ji, Sixun Peng, Yihua Zhang*. Design, synthesis and evaluation of nitric oxide releasing derivatives of 3-n-butylphthalide as antiplatelet and antithrombotic agents. Org Biomol Chem, 2011, 9(16): 5670-5681.

  39. Yang Li, Xuliang Wang, Rong Fu, Wenying Yu, Xiaoli Wang, Yisheng Lai, Sixun Peng, Yihua Zhang*. Synthesis and evaluation of nitric oxide-releasing derivatives of 3-n-butylphthalide as anti-platelet agents. Bioorg Med Chem Lett, 2011, 21(14): 4210-4214.

  40. Lihong Shen*, Ya Li, Dahai Zhang, Yisheng Lai, Lijie Liu. Synthesis and evaluation of nitrate derivatives of colchicine as anticancer agents. Chin Chem Lett, 2011, 22(7): 768-770.

  41. Yisheng Lai*, Lin Ma, Wenxing Huang, Xing Yu, Yihua Zhang, Hui Ji*, Jide Tian. Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)phenyl]methylene- indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors.Bioorg Med Chem Lett, 2010, 20(24): 7349-7353.

  42. Yisheng Lai*, Lihong Shen, Zhenzhen Zhang, Wenqing Liu, Yihua Zhang, Hui Ji*, Jide Tian. Synthesis and biological evaluation of furoxan-based nitric oxide-releasing derivatives of glycyrrhetinic acid as anti-hepatocellular carcinoma agents.Bioorg Med Chem Lett, 2010, 20(22): 6416-6420.

  43. Xiaolei YeWu ZhouYongqi LiYihua SunYihua ZhangHui Ji*, Yisheng Lai*. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol, 2010, 66(2): 277-285.

  44. Zhangjian Huang, Yihua Zhang*, Li Zhao, Yongwang Jing, Yisheng Lai, Luyong Zhang, Qinglong Guo, Shengtao Yuan, Jianjun Zhang, Li Chen, Sixun Peng and Jide Tian. Synthesis and anti-human hepatocellular carcinoma activity of new nitric oxide-releasing glycosyl derivatives of oleanolic acid.Org Biomol Chem, 2010, 8(3): 632-639.

  45. Yong Ling, Xiaolei Ye, Hui Ji*, Yihua Zhang*, Yisheng Lai, Sixun Peng, Jide Tian. Synthesis and evaluation of nitric oxide-releasing derivatives of farnesylthiosalicylic acid as anti-tumor agents.Bioorg Med Chem, 2010, 18(10): 3448-3456.