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Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres. | LitMetric
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Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.

Frederick Cohen Michael F T Koehler Philippe Bergeron Linda O Elliott John A Flygare Matthew C Franklin Lewis Gazzard Stephen F Keteltas Kevin Lau Cuong Q Ly Vickie Tsui Wayne J Fairbrother

Bioorg Med Chem Lett

Department of Discovery Chemistry, Genentech, Inc. 1 DNA Way, South San Francisco, CA 94080, USA.

Published: April 2010

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.

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http://dx.doi.org/10.1016/j.bmcl.2010.02.021DOI Listing

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