[10-11]Synthesis of triterpene derivatives as potent Wild-Type and Bevirimat-Resistant HIV-1 Maturation Inhibitors

报告题目:Synthesis of triterpene derivatives as potent Wild-Type and Bevirimat-Resistant HIV-1 Maturation Inhibitors

报 告 人:陈重(苏州大学药学院  助理研究员)
报告时间:20171011日(星期三)下午3:00
报告地点:独墅湖校区二期云轩楼2301

 

报告摘要:
Bevirimat, 3-O-(3’,3’-Dimethylsuccinyl) betulinic acid, was firstly identified as the HIV-1 maturation inhibitor (MI) by Dr. Lee’s group in UNC at Chapel Hill, which was approved into Phase Ⅱb clinical trial by FDA. As a first-in-class MI, the unique features of Bevirimat have promoted several industry groups (including GSK, Bristol-Myers Squibb, Pfizer) to develop second-generation HIV-1 MIs with the primary goal of overcoming the challenge of drug resistance associated with naturally occurring Gag polymorphisms that has halted further clinical development of Bevirimat. With Bevirimat as the lead compound, we designed, synthesized and evaluated the anti-HIV-1 activity of 40 triterpene derivatives, including Wild-Type and Bevirimat-Resistant HIV-1 strains. This report will disclose the new SAR on triterpenes, which is helpful to develop the next generation MIs. Moreover, this report will illustrate how to discover and develop new drug based on natural product with Bevirimat as a living example.

 

报告人简介:
陈重,2015年毕业于苏州大学,获药学博士(天然药物化学方向)。2016.6-2017.9在美国University of North Carolina at Chapel Hill以访问学者身份从事抗HIV-1和抗肿瘤方面的研究。现为苏州大学药学院助理研究员,主要从事活性天然产物的结构修饰与构效关系(SAR)研究、抗肿瘤新靶点(如VEGFR, EGFR等)与新作用机制研究、抗HIV-1天然产物研究。近三年来主持国家自然科学基金青年基金项目1项,主持江苏省高校自然科学基金面上项目1项,主持江苏省研究生创新工程项目1项, 在 J. Nat. Prod.,  Eur. J. Med. Chem.,  J. Org. Chem Org. Biomol. Chem. 等期刊 发表学术论文20余篇,其中以第一作者或通讯作者发表SCI 论文7篇(其中SCI 2区论文3 篇)。申请中国发明专利8份,其中授权5份。