title: Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
abstract: Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.
authors.affiliation: Department of Chemistry, Tanabe Research Laboratories USA, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA.
authors.forename: Madhavi
authors.initials: M
authors.lastname: Pannala
authors.forename: Sunil
authors.initials: S
authors.lastname: Kher
authors.forename: Norma
authors.initials: N
authors.lastname: Wilson
authors.forename: John
authors.initials: J
authors.lastname: Gaudette
authors.forename: Ila
authors.initials: I
authors.lastname: Sircar
authors.forename: Shao-Hui
authors.initials: SH
authors.lastname: Zhang
authors.forename: Alexei
authors.initials: A
authors.lastname: Bakhirev
authors.forename: Guang
authors.initials: G
authors.lastname: Yang
authors.forename: Phoebe
authors.initials: P
authors.lastname: Yuen
authors.forename: Frank
authors.initials: F
authors.lastname: Gorcsan
authors.forename: Naoki
authors.initials: N
authors.lastname: Sakurai
authors.forename: Miguel
authors.initials: M
authors.lastname: Barbosa
authors.forename: Jie-Fei
authors.initials: JF
authors.lastname: Cheng
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D009570:Nitriles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship