Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 7, Pages 2229-2233Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.021
Keywords
IAP antagonist; Peptidomimetic; Protein-protein interaction
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Funding
- Genentech Discovery Chemistry
- Department of Energy
- Office of Biological and Environmental Research
- National Institutes of Health
- National Center for Research Resources
- Biomedical Technology Program
- National Institute of General Medical Sciences
- US Department of Energy [DE-AC0-205CH11231]
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A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3. (C) 2010 Elsevier Ltd. All rights reserved.
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