title: Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.
abstract: The structure-activity relationship of a novel subseries of 4-anilinoquinazoline EGFR inhibitors substituted at the C-6 position with carbon-linked side chains has been investigated. This exploration has led to the discovery of novel aminomethyl carboxamides with good biological, pharmacokinetic and physical properties.
authors.affiliation: AstraZeneca, Centre de Recherches, Z.I. La Pompelle, B.P. 1050, Chemin de Vrilly, 51689 Reims, Cedex 2, France. Laurent.Hennequin@astrazeneca.com
authors.forename: Laurent F A
authors.initials: LF
authors.lastname: Hennequin
authors.forename: Peter
authors.initials: P
authors.lastname: Ballard
authors.forename: F Tom
authors.initials: FT
authors.lastname: Boyle
authors.forename: Bénédicte
authors.initials: B
authors.lastname: Delouvrié
authors.forename: Rebecca P A
authors.initials: RP
authors.lastname: Ellston
authors.forename: Chris T
authors.initials: CT
authors.lastname: Halsall
authors.forename: Craig S
authors.initials: CS
authors.lastname: Harris
authors.forename: Kevin
authors.initials: K
authors.lastname: Hudson
authors.forename: Jane
authors.initials: J
authors.lastname: Kendrew
authors.forename: J Elizabeth
authors.initials: JE
authors.lastname: Pease
authors.forename: Helen S
authors.initials: HS
authors.lastname: Ross
authors.forename: Peter
authors.initials: P
authors.lastname: Smith
authors.forename: Jennifer L
authors.initials: JL
authors.lastname: Vincent
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004285:Dogs; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D011799:Quinazolines; D066246:ErbB Receptors