Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 3, Pages 593-596Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm801101z
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Funding
- Chinese Academy of Sciences
- National Natural Science Foundation of China [20620120106, 20621062, 90713047]
- U.S. National Cancer Institute
- National Institutes of Health [R01CA109025]
- Breast Cancer Research Foundation
- Susan G. Konien Foundation
- Prostate Cancer Foundation
- University of Michigan Cancer Center [P30CA046592]
- Ascenta Therapeutics, Inc.
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A series of new Smac mimetics have been designed, synthesized, and evaluated. The most potent compound 10 binds to XIAP, cIAP-1, and cIAP-2 BIR3 proteins with K-i of 3.9, 0.37, and 0.25 nM, respectively. Compound 10 antagonizes XIAP in a cell-free functional assay and induces rapid cIAP-1 degradation in cancer cells. Compound 10 inhibits cell growth in the MDA-MB-231 cancer cell line with an IC50 of 8.9 nM.
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