Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors

详细信息    查看全文

• 作者：Huansheng Fu ; Xuben Hou ; Lei Wang ; Yanyan Dun ; Xinying Yang ; Hao Fang ; ^{haofangcn@sdu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Apoptosis ; Bcl-2 ; Inhibitor ; Rhodanine
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：15 November 2015
• 年：2015
• 卷：25
• 期：22
• 页码：5265-5269
• 全文大小：815 K

文摘

A new class of 3-aryl-rhodanine benzoic acid derivatives were designed, synthesized, and evaluated for their inhibition activities against anti-apoptotic Bcl-2 proteins. The potent compounds 33 and 41 bound to Bcl-2 with submicromolar K_i values and had selectivities to Bcl-2/Mcl-1 over Bcl-xL. In addition, they exhibited obvious antiproliferative activities in three human tumor cell lines (MDA-MB-231, K562 and PC-3).