title: 7-(aryl/heteroaryl-2-ylethynyl)-4-phenylamino-3-quinolinecarbonitriles as new Src kinase inhibitors: addition of water solubilizing groups.
abstract: New 4-phenylamino-3-quinolinecarbonitriles with a 7-ethynyl group substituted by a pyridine, phenyl or thiophene ring containing basic water solubilizing groups were prepared and evaluated as Src kinase inhibitors. Of these new analogs, potent activity was observed with compounds having a (2,4-dichloro-5-methoxyphenyl)amino group at C-4, a methoxy or ethoxy group at C-6, and a pyridyl group bearing a dimethylamine or N-methylpiperazine on the ethynyl group at C-7.
authors.affiliation: Department of Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. wub@wyeth.com
authors.forename: Biqi
authors.initials: B
authors.lastname: Wu
authors.forename: Ana Carolina
authors.initials: AC
authors.lastname: Barrios Sosa
authors.forename: Diane H
authors.initials: DH
authors.lastname: Boschelli
authors.forename: Frank
authors.initials: F
authors.lastname: Boschelli
authors.forename: Erick E
authors.initials: EE
authors.lastname: Honores
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Golas
authors.forename: Dennis W
authors.initials: DW
authors.lastname: Powell
authors.forename: Yanong D
authors.initials: YD
authors.lastname: Wang
mesh_terms: D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D014867:Water / Q000737:chemistry*; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
chemical_list: D011804:Quinolines; D014867:Water; D019061:src-Family Kinases