Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors.
A series of substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles has been prepared as Src kinase inhibitors. Optimal activity is observed with compounds that have basic amines attached via the para position of the 7-phenyl ring, and a hydrogen atom at the C-6 position. The best compounds are low nanomolar inhibitors of Src kinase, and have potent activity against Src-transformed fibroblast cells.
Berger
Dan
D
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA. bergerd@wyeth.com
Dutia
Minu
M
Powell
Dennis
D
Wissner
Allan
A
DeMorin
Frenel
F
Raifeld
Yuri
Y
Weber
Jennifer
J
Boschelli
Frank
F
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D009570:Nitriles; D011804:Quinolines; D019061:src-Family Kinases