Synthesis and Src kinase inhibitory activity of a series of 4-[(2, 4-dichloro-5-methoxyphenyl) amino]-7-furyl-3-quinolinecarbonitriles

…, Y Wang, JM Golas, J Lucas, F Boschelli

Index: Boschelli, Diane H.; Wu, Biqi; Ye, Fei; Wang, Yan; Golas, Jennifer M.; Lucas, Judy; Boschelli, Frank Journal of Medicinal Chemistry, 2006 , vol. 49, # 26 p. 7868 - 7876

Full Text: HTML

Citation Number: 30

Abstract

Compound 1 (SKI-606, bosutinib), a 7-alkoxy-4-[(2, 4-dichloro-5-methoxyphenyl) amino]-3- quinolinecarbonitrile, is a potent inhibitor of Src kinase activity. We previously reported that analogs of 1 with thiophene groups at C-7 retained the Src activity of the parent compound. The corresponding C-7 furan analogs were prepared and it was found that the 3, 5- substituted furan analog had increased activity compared to that of the 2, 5-substituted ...