7-(aryl/heteroaryl-2-ylethynyl)-4-phenylamino-3-quinolinecarbonitriles as new Src kinase inhibitors: addition of water solubilizing groups.
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.
Wu
Biqi
B
Department of Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. wub@wyeth.com
Barrios Sosa
Ana Carolina
AC
Boschelli
Diane H
DH
Boschelli
Frank
F
Honores
Erick E
EE
Golas
Jennifer M
JM
Powell
Dennis W
DW
Wang
Yanong D
YD
D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D014867:Water / Q000737:chemistry*; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D011804:Quinolines; D014867:Water; D019061:src-Family Kinases