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

  1. Author:
    Tang, G. Z.
    Yang, C. Y.
    Nikolovska-Coleska, Z.
    Guo, J.
    Qiu, S.
    Wang, R. X.
    Gao, W.
    Wang, G. P.
    Stuckey, J.
    Krajewski, K.
    Jiang, S.
    Roller, P. P.
    Wang, S. M.
  2. Author Address

    Univ Michigan, Dept Internal Med, Ann Arbor, MI 48109 USA. Univ Michigan, Dept Pharmacol & Med Chem, Ctr Comprehens Canc, Ann Arbor, MI 48109 USA. Univ Michigan, Inst Life Sci, Ann Arbor, MI 48109 USA. NCI, Med Chem Lab, NIH, Frederick, MD 21702 USA.;Wang, SM, Univ Michigan, Dept Internal Med, 1500 E Med CTr Dr, Ann Arbor, MI 48109 USA.;shaomeng@umich.edu
    1. Year: 2007
    2. Date: Apr
  1. Journal: Journal of Medicinal Chemistry
    1. 50
    2. 8
    3. Pages: 1723-1726
  2. Type of Article: Article
  3. ISSN: 0022-2623
  1. 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 K-i 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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External Sources

  1. DOI: 10.1021/jm0614001
  2. WOS: 000245634500001

Library Notes

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