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

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.
AuthorsGuozhi 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
JournalJournal of medicinal chemistry (J Med Chem) Vol. 50 Issue 8 Pg. 1723-6 (Apr 19 2007) ISSN: 0022-2623 [Print] United States
PMID17378545 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)
Chemical References
  • Antineoplastic Agents
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Neoplasm Proteins
  • Proto-Oncogene Proteins c-bcl-2
  • bcl-X Protein
  • Pyrogallol
Topics
  • Antineoplastic Agents (chemical synthesis, pharmacology)
  • Apoptosis
  • Binding, Competitive
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Models, Molecular
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Neoplasm Proteins (antagonists & inhibitors)
  • Proto-Oncogene Proteins c-bcl-2 (antagonists & inhibitors)
  • Pyrogallol (analogs & derivatives, chemical synthesis, pharmacology)
  • Radioligand Assay
  • Structure-Activity Relationship
  • bcl-X Protein (antagonists & inhibitors)

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