Pyrogallol-Based Molecules as Potent Inhibitors of the Antiapoptotic Bcl-2 Proteins
Journal of Medicinal Chemistry2007Vol. 50(8), pp. 1723–1726
Citations Over TimeTop 15% of 2007 papers
Guozhi Tang, Chao‐Yie Yang, Zaneta Nikolovska‐Coleska, Jie Guo, Su Qiu, Renxiao Wang, Wei Gao, Guoping Wang, Jeanne A. Stuckey, Krzysztof Krajewski, Sheng Jiang, Peter P. Roller, Shaomeng Wang
Abstract
We report herein a new class of small-molecule inhibitors of antiapoptotic Bcl-2 proteins. The most potent compound, 7, binds to Bcl-2, Bcl-xL, and Mcl-1 proteins with Ki of 110, 638, and 150 nM, respectively. Compound 7 is highly effective in induction of cell death in breast cancer cells with high levels of Bcl-2, Bcl-xL, and Mcl-1 proteins and represents a promising lead compound for the design of new anticancer drugs.
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