Department of Discovery Chemistry, Genentech, Inc. 1 DNA Way, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. doi: 10.1016/j.bmcl.2010.02.021. Epub 2010 Feb 8.
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.
设计并合成了一系列基于噻唑或苯并噻唑酰胺等排体的 IAP 拮抗剂。这些化合物通过荧光偏振测定法被测试了与 XIAP-BIR3 和 ML-IAP BIR 的结合能力。其中最有效的两种化合物 19a 和 33b，对 ML-IAP 的 K(i)值为 20-30 nM，对 XIAP-BIR3 的 K(i)值为 50-60 nM。
