title: Identification of selective inhibitors of cyclin dependent kinase 4.
abstract: A new structural type of kinase inhibitor, containing a benzocarbazole nucleus, has been identified. Members of the series are selective for inhibition of the cyclin dependent kinase family of enzymes. Although the cdks are highly homologous, representatives of the series showed intra-cdk selectivities, especially for cdk4. SAR studies elucidated the important features of the molecules for inhibition.
authors.affiliation: DuPont Pharmaceuticals Company, Wilmington, DE 19880, USA. thais.m.sielecki@dupontpharma.com
authors.forename: D J
authors.initials: DJ
authors.lastname: Carini
authors.forename: R F
authors.initials: RF
authors.lastname: Kaltenbach
authors.forename: J
authors.initials: J
authors.lastname: Liu
authors.forename: P A
authors.initials: PA
authors.lastname: Benfield
authors.forename: J
authors.initials: J
authors.lastname: Boylan
authors.forename: M
authors.initials: M
authors.lastname: Boisclair
authors.forename: L
authors.initials: L
authors.lastname: Brizuela
authors.forename: C R
authors.initials: CR
authors.lastname: Burton
authors.forename: S
authors.initials: S
authors.lastname: Cox
authors.forename: R
authors.initials: R
authors.lastname: Grafstrom
authors.forename: B A
authors.initials: BA
authors.lastname: Harrison
authors.forename: K
authors.initials: K
authors.lastname: Harrison
authors.forename: E
authors.initials: E
authors.lastname: Akamike
authors.forename: J A
authors.initials: JA
authors.lastname: Markwalder
authors.forename: Y
authors.initials: Y
authors.lastname: Nakano
authors.forename: S P
authors.initials: SP
authors.lastname: Seitz
authors.forename: D M
authors.initials: DM
authors.lastname: Sharp
authors.forename: G L
authors.initials: GL
authors.lastname: Trainor
authors.forename: T M
authors.initials: TM
authors.lastname: Sielecki
mesh_terms: D002227:Carbazoles / Q000737:chemistry / Q000494:pharmacology*; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D011518:Proto-Oncogene Proteins; D013329:Structure-Activity Relationship
chemical_list: D002227:Carbazoles; D004791:Enzyme Inhibitors; D011518:Proto-Oncogene Proteins; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases