Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins
Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins
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DOI：
10.1021/jm701358v
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发表时间：
2008-02-28
影响因子：
7.3
通讯作者：
Wang, Shaomeng
中科院分区：
文献类型：
--
作者：
Tang, Guozhi;Nikolovska-Coleska, Zaneta;Wang, Shaomeng
设计、合成了一系列酰基焦性没食子酚类化合物，并对其作为抗凋亡Bcl-2蛋白的小分子抑制剂进行了评价。最有效的化合物9（TM-179）以170 nM的IC 50结合Bcl-2，以37 nM的Ki结合Mcl-1。化合物9有效抑制人乳腺癌和前列腺癌细胞系中的细胞生长并诱导细胞凋亡。
A series of acylpyrogallols were designed, synthesized, and evaluated as small-molecule inhibitors of antiapoptotic Bcl-2 proteins. The most potent compound 9 (TM-179) binds to Bcl-2 with an IC50 of 170 nM and to Mcl-1 with a K-i of 37 nM. Compound 9 potently inhibits cell growth and induces apoptosis in human breast and prostate cancer cell lines.