CN
- Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase γ inhibitors.
Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase γ inhibitors.
Bioorganic & medicinal chemistry letters (2012-11-06)
Yusuke Oka, Tetsuya Yabuuchi, Yasuyuki Fujii, Hidenori Ohtake, Shunichi Wakahara, Kayo Matsumoto, Mayumi Endo, Yunoshin Tamura, Yoshinori Sekiguchi
PMID23122859
摘要
A novel series of 2-aminothiazole-oxazoles was designed and synthesized as part of efforts to develop potent phosphoinositide 3-kinase γ (PI3Kγ) 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.
材料