Article
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Journal of medicinal chemistry - 13 May 2010
Feng Yu, Ding Xiao, Chen Tao, Chen Lili, Liu Fang, Jia Xu, Luo Xiaomin, Shen Xu, Chen Kaixian, Jiang Hualiang, Wang Hui, Liu Hong, Liu Dongxiang
Abstract excerpt
Development of inhibitors to antagonize the activities of antiapoptotic Bcl-2 family proteins is of particular interest in cancer chemotherapy. We discovered a quinazoline-2(1H)-thione derivative (DCBL55) as a new Bcl-x(L), Bcl-2, and Mcl-1 inhibitor by virtual database screening. We systematically modified the structure of compound 1 by chemical synthesis. The interactions of the compounds with Bcl-x(L) were...
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