Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927

DH Boschelli, ACB Sosa, JM Golas…

Index: Boschelli, Diane H.; Barrios Sosa, Ana Carolina; Golas, Jennifer M.; Boschelli, Frank Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 5 p. 1358 - 1361

Full Text: HTML

Citation Number: 16

Abstract

Of a series of 7-ethynyl-3-quinolinecarbonitriles, the most potent Src inhibitory activity was observed with 4-[(2, 4-dichloro-5-methoxyphenyl) amino]-6-methoxy-7-[4-(4-methylpiperazin- 1-yl) but-1-ynyl]-3-quinolinecarbonitrile (SKS-927). Variation of the solubilizing amine tail or removal of the methoxy group from either C-6 of the quinoline core or C-5 of the aniline headpiece led to reduced activity.