Acylpyrogallols as Inhibitors of Antiapoptotic Bcl-2 Proteins

Tang, Guozhi; Nikolovska-Coleska, Zaneta; Qiu, Su; Yang, Chao-Yie; Guo, Jie; Wang, Shaomeng

doi:10.1021/jm701358v.s001

jm701358v_si_001.pdf (139.24 kB)

Acylpyrogallols as Inhibitors of Antiapoptotic Bcl-2 Proteins

journal contribution

posted on 2008-02-28, 00:00 authored by Guozhi Tang, Zaneta Nikolovska-Coleska, Su Qiu, Chao-Yie Yang, Jie Guo, Shaomeng Wang

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.