|
|||||
|
|
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres |
|
| Authors: | Frederick Cohen Michael FT 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 |
| Institution: | 1. Department of Discovery Chemistry, Genentech, Inc. 1 DNA Way, South San Francisco, CA 94080, USA;2. Department of Biochemical Pharmacology, 1 DNA Way, South San Francisco, CA 94080, USA;3. Department of Protein Engineering Genentech, Inc. 1 DNA Way, South San Francisco, CA 94080, USA |
| Abstract: | 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 Ki’s of 20–30 nM against ML-IAP and 50–60 nM against XIAP-BIR3. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |