期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 6, 页码 1723-1730出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801450c
关键词
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资金
- U.S. Department of Energy
- National Institutes of Health
A series of IAP antagonists based on an azabicyclooctane scaffold was designed and synthesized. The most potent of these compounds, 14b, binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domain of c-IAP1 with K(i) values of 140, 38, and 33 nM, respectively. These compounds promote degradation of c-IAP1, activate caspases, and lead to decreased viability of breast cancer cells without affecting normal mammary epithelial cells. Finally, compound 14b inhibits tumor growth when dosed orally in a breast cancer xenograft model.
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