Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
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ABSTRACT:
SUBMITTER: Tang G
PROVIDER: S-EPMC2536619 | biostudies-literature | 2007 Apr
REPOSITORIES: biostudies-literature
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Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
Tang Guozhi G Yang Chao-Yie CY Nikolovska-Coleska Zaneta Z Guo Jie J Qiu Su S Wang Renxiao R Gao Wei W Wang Guoping G Stuckey Jeanne J Krajewski Krzysztof K Jiang Sheng S Roller Peter P PP Wang Shaomeng S
Journal of medicinal chemistry 20070323 8
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. ...[more]
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