Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity

DH Boschelli, F Ye, YD Wang, M Dutia…

文献索引：Boschelli; Wang; Ye; Wu; Zhang; Dutia; Powell; Wissner; Arndt; Weber Journal of Medicinal Chemistry, 2001 , vol. 44, # 5 p. 822 - 833

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被引用次数: 171

摘要

Subsequent to the discovery of 4-[(2, 4-dichlorophenyl) amino]-6, 7-dimethoxy-3- quinolinecarbonitrile (1a) as an inhibitor of Src kinase activity (IC50= 30 nM), several additional analogues were prepared. Optimization of the C-4 anilino group of 1a led to 1c, which contains a 2, 4-dichloro-5-methoxy-substituted aniline. Replacement of the methoxy group at C-7 of 1c with a 3-(morpholin-4-yl) propoxy group provided 2c, resulting in ...