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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Authors | 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 |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 50
Issue 8
Pg. 1723-6
(Apr 19 2007)
ISSN: 0022-2623 [Print] United States |
PMID | 17378545
(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.)
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Chemical References |
- Antineoplastic Agents
- Myeloid Cell Leukemia Sequence 1 Protein
- Neoplasm Proteins
- Proto-Oncogene Proteins c-bcl-2
- bcl-X Protein
- Pyrogallol
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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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