title: Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles.
abstract: A series of 7-ethynyl and 7-ethenyl-4-anilino-3-quinolinecarbonitriles were synthesized and tested for Src inhibition. Derivatives bearing a C-6 methoxy group and 2,4-dichloro-5-methoxyaniline at C-4 showed optimal inhibition of Src enzymatic and cellular activity. The ethenyl and ethynyl groups were incorporated at C-7 utilizing a Stille, Heck, or Sonogashira coupling reaction.
authors.affiliation: Wyeth Research, Chemical and Screening Sciences, 401 N. Middletown Road, Pearl River, NY 10965, USA. barrioal@wyeth.com
authors.forename: Ana Carolina
authors.initials: AC
authors.lastname: Barrios Sosa
authors.forename: Diane H
authors.initials: DH
authors.lastname: Boschelli
authors.forename: Fei
authors.initials: F
authors.lastname: Ye
authors.forename: Jennifer M
authors.initials: JM
authors.lastname: Golas
authors.forename: Frank
authors.initials: F
authors.lastname: Boschelli
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009570:Nitriles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D009570:Nitriles; D019061:src-Family Kinases