Structure-Based Design of Flavonoid Compounds As a New Class of Small-Molecule Inhibitors of the Anti-apoptotic Bcl-2 Proteins
Journal of Medicinal Chemistry2007Vol. 50(14), pp. 3163–3166
Citations Over TimeTop 14% of 2007 papers
Guozhi Tang, Ke Ding, Zaneta Nikolovska‐Coleska, Chao‐Yie Yang, Su Qiu, Sanjeev Shangary, Renxiao Wang, Jie Guo, Wei Gao, Jennifer L. Meagher, Jeanne A. Stuckey, Krzysztof Krajewski, Sheng Jiang, Peter P. Roller, Shaomeng Wang
Abstract
Structure-based strategy was employed to design flavonoid compounds to mimic the Bim BH3 peptide as a new class of inhibitors of the anti-apoptotic Bcl-2 proteins. The most potent compound, 4 (BI-33), binds to Bcl-2 and Mcl-1 with Ki values of 17 and 18 nM, respectively. Compound 4 inhibits cell growth in the MDA-MB-231 breast cancer cell line with an IC50 value of 110 nM and effectively induces apoptosis.
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