title: Quinazolines as cyclin dependent kinase inhibitors.
abstract: Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase, parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined.
authors.affiliation: The DuPont Pharmaceuticals Company, Wilmington, DE 19880-0500, USA. thais.m.sielecki@dupontpharma.com
authors.forename: T M
authors.initials: TM
authors.lastname: Sielecki
authors.forename: T L
authors.initials: TL
authors.lastname: Johnson
authors.forename: J
authors.initials: J
authors.lastname: Liu
authors.forename: J K
authors.initials: JK
authors.lastname: Muckelbauer
authors.forename: R H
authors.initials: RH
authors.lastname: Grafstrom
authors.forename: S
authors.initials: S
authors.lastname: Cox
authors.forename: J
authors.initials: J
authors.lastname: Boylan
authors.forename: C R
authors.initials: CR
authors.lastname: Burton
authors.forename: H
authors.initials: H
authors.lastname: Chen
authors.forename: A
authors.initials: A
authors.lastname: Smallwood
authors.forename: C H
authors.initials: CH
authors.lastname: Chang
authors.forename: M
authors.initials: M
authors.lastname: Boisclair
authors.forename: P A
authors.initials: PA
authors.lastname: Benfield
authors.forename: G L
authors.initials: GL
authors.lastname: Trainor
authors.forename: S P
authors.initials: SP
authors.lastname: Seitz
mesh_terms: D001667:Binding, Competitive / Q000187:drug effects; D002460:Cell Line; D018360:Crystallography, X-Ray; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D011799:Quinazolines / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011799:Quinazolines; D018844:Cyclin-Dependent Kinases