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Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins. | LitMetric
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Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.

Guozhi Tang Chao-Yie Yang Zaneta Nikolovska-Coleska Jie Guo Su Qiu Renxiao Wang Wei Gao Guoping Wang Jeanne Stuckey Krzysztof Krajewski Sheng Jiang Peter P Roller Shaomeng Wang

J Med Chem

Department of Internal Medicine, Comprehensive Cancer Center, and Life Sciences Institute, University of Michigan, 1500 East Medical Center Drive, Ann Arbor, Michigan 48109, USA.

Published: April 2007

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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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2536619PMC
http://dx.doi.org/10.1021/jm061400lDOI Listing

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