Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors

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• 作者：Jongkook Lee^a ; ^b ; Sun-Young Han^a ; ^c ; Heejung Jung^a ; Jeon Yang^a ; ^d ; Jie-Won Choi^a ; ^e ; Chong Hack Chae^a ; Chi Hoon Park^a ; Sang Un Choi^a ; Kwangho Lee^a ; Jae Du Ha^a ; Chong Ock Lee^a ; Jae Wook Ryu^a ; Hyoung Rae Kim^a ; Jong Sung Koh^a ; Sung Yun Cho^a ; ^{sycho@krict.re.kr}
• 关键词：Cancer ; c-Met kinase ; Aminopyridine ; Benzoxazole
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 June, 2012
• 卷：22
• 期：12
• 页码：4044-4048
• 文件大小：476 K

摘要

A series of hydroxybenzoxazole derivatives was synthesized, and their c-Met kinase inhibitory activity was evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent benzoxazole scaffold, with particular focus on the hydroxyl substituent of the benzoxazole moiety.