3-芳基罗丹宁苯甲酸作为抗凋亡蛋白Bcl-2抑制剂的设计、合成及生物学评价
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.
作者信息
Fu Huansheng, Hou Xuben, Wang Lei, Dun Yanyan, Yang Xinying, Fang Hao
机构信息
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Rd, Ji'nan 250012, PR China.
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Rd, Ji'nan 250012, PR China.
出版信息
Bioorg Med Chem Lett. 2015 Nov 15;25(22):5265-9. doi: 10.1016/j.bmcl.2015.09.051. Epub 2015 Sep 25.
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 Ki 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).
设计、合成了一类新型的3-芳基罗丹宁苯甲酸衍生物，并对其抗凋亡Bcl-2蛋白的抑制活性进行了评估。强效化合物33和41与Bcl-2结合，Ki值为亚微摩尔级别，对Bcl-2/Mcl-1的选择性高于Bcl-xL。此外，它们在三种人类肿瘤细胞系（MDA-MB-231、K562和PC-3）中表现出明显的抗增殖活性。
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