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Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins |
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| Authors: | Tang Guozhi Nikolovska-Coleska Zaneta Qiu Su Yang Chao-Yie Guo Jie Wang Shaomeng |
| Abstract: | 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 Ki of 37 nM. Compound 9 potently inhibits cell growth and induces apoptosis in human breast and prostate cancer cell lines. |
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