title: Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors.
abstract: 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.
authors.affiliation: Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA. bergerd@wyeth.com
authors.forename: Dan
authors.initials: D
authors.lastname: Berger
authors.forename: Minu
authors.initials: M
authors.lastname: Dutia
authors.forename: Dennis
authors.initials: D
authors.lastname: Powell
authors.forename: Allan
authors.initials: A
authors.lastname: Wissner
authors.forename: Frenel
authors.initials: F
authors.lastname: DeMorin
authors.forename: Yuri
authors.initials: Y
authors.lastname: Raifeld
authors.forename: Jennifer
authors.initials: J
authors.lastname: Weber
authors.forename: Frank
authors.initials: F
authors.lastname: Boschelli
mesh_terms: 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*
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D009570:Nitriles; D011804:Quinolines; D019061:src-Family Kinases