Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins

作者：Tang Guozhi; Nikolovska Coleska Zaneta; Qiu Su; Yang Chao Yie; Guo Jie; Wang Shaomeng^*

来源：Journal of Medicinal Chemistry, 2008, 51(4): 717-720.

DOI：10.1021/jm701358v

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.

• 出版日期2008-2-28