4.5 Article

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 7, 页码 2229-2233

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.02.021

关键词

IAP antagonist; Peptidomimetic; Protein-protein interaction

资金

  1. Genentech Discovery Chemistry
  2. Department of Energy
  3. Office of Biological and Environmental Research
  4. National Institutes of Health
  5. National Center for Research Resources
  6. Biomedical Technology Program
  7. National Institute of General Medical Sciences
  8. US Department of Energy [DE-AC0-205CH11231]

向作者/读者索取更多资源

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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