Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase γ inhibitors
作者:Yusuke Oka、Tetsuya Yabuuchi、Yasuyuki Fujii、Hidenori Ohtake、Shunichi Wakahara、Kayo Matsumoto、Mayumi Endo、Yunoshin Tamura、Yoshinori Sekiguchi
DOI:10.1016/j.bmcl.2012.10.028
日期:2012.12
A novel series of 2-aminothiazole-oxazoles was designed and synthesized as part of efforts to develop potent phosphoinositide 3-kinase gamma (PI3K gamma) inhibitors. The modification of a high-throughput screening hit, compound 1, resulted in the identification of compounds 10 and 15, which displayed potent inhibitory activities in enzyme-based and cell-based assays. (C) 2012 Elsevier Ltd. All rights reserved.