2. Academic Validation
  3. Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins

Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins

  • J Med Chem. 2008 Feb 28;51(4):717-20. doi: 10.1021/jm701358v.
Guozhi Tang,  Zaneta Nikolovska-Coleska,  Su Qiu,  Chao-Yie Yang,  Jie Guo,  Shaomeng Wang
PMID: 18237106 DOI: 10.1021/jm701358v
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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