title: Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.
abstract: The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC(50) values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.
authors.affiliation: Wyeth Research, Chemical Sciences 401 N. Middletown Road, Pearl River, NY 10965, United States. bosched@wyeth.com
authors.forename: Diane H
authors.initials: DH
authors.lastname: Boschelli
authors.forename: Daniel
authors.initials: D
authors.lastname: Wang
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.forename: Biqi
authors.initials: B
authors.lastname: Wu
authors.forename: Erick E
authors.initials: EE
authors.lastname: Honores
authors.forename: Ana Carolina
authors.initials: AC
authors.lastname: Barrios Sosa
authors.forename: Inder
authors.initials: I
authors.lastname: Chaudhary
authors.forename: Jennifer
authors.initials: J
authors.lastname: Golas
authors.forename: Judy
authors.initials: J
authors.lastname: Lucas
authors.forename: Frank
authors.initials: F
authors.lastname: Boschelli
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D008861:Microsomes / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays; D019061:src-Family Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011804:Quinolines; D019061:src-Family Kinases