Discovery of N-((4-([1, 2, 4] Triazolo [1, 5-a] pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1 H-imidazol-2-yl) methyl)-2-fluoroaniline (EW-7197): A Highly Potent, Selective, and …

…, D Sreenu, VB Subrahmanyam, KS Rao…

文献索引：Jin, Cheng Hua; Krishnaiah, Maddeboina; Sreenu, Domalapally; Subrahmanyam, Vura B.; Rao, Kota S.; Lee, Hwa Jeong; Park, So-Jung; Park, Hyun-Ju; Lee, Kiho; Sheen, Yhun Yhong; Kim, Dae-Kee Journal of Medicinal Chemistry, 2014 , vol. 57, # 10 p. 4213 - 4238

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被引用次数: 16

摘要

A series of 2-substituted-4-([1, 2, 4] triazolo [1, 5-a] pyridin-6-yl)-5-(6-methylpyridin-2-yl) imidazoles was synthesized and evaluated to optimize a prototype inhibitor of TGF-β type I receptor kinase (ALK5), 6. Combination of replacement of a quinoxalin-6-yl moiety of 6 with a [1, 2, 4] triazolo [1, 5-a] pyridin-6-yl moiety, insertion of a methyleneamino linker, and ao-F substituent in the phenyl ring markedly increased ALK5 inhibitory activity, kinase ...