Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors

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• 作者：Sun-Young Han^a ; ^b ; Jie Won Choi^a ; ^c ; Jeon Yang^a ; ^d ; Chong Hack Chae^a ; Jongkook Lee^a ; Heejung Jung^a ; Kwangho Lee^a ; Jae Du Ha^a ; ; Hyoung Rae Kim^a ; Sung Yun Cho^a ; ^{sycho@krict.re.kr}
• 关键词：Cancer ; VEGFR-2 ; KDR kinase ; Imidazo[4 ; 5-c]pyridine ; Quinolin-2-one
• 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 April, 2012
• 卷：22
• 期：8
• 页码：2837-2842
• 文件大小：3021 K

摘要

A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic acid ethyl esters were synthesized, and their VEGFR-2 inhibitory activity was evaluated. Described herein are the preparation of the series and the effects of the compounds on VEGFR-2 kinase activity.