title: Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.
abstract: A series of 2-anilino-4-(1H-pyrrol-3-yl)pyrimidines were prepared and evaluated for their ability to inhibit cyclin-dependent kinases (CDKs). A number of analogues were found to be potent CDK2 and CDK4 inhibitors and to exhibit anti-proliferative activity against human tumour cell lines. Structure-activity relationships and biochemical characterization are presented.
authors.affiliation: Cyclacel Limited, James Lindsay Place, Dundee DD1 5JJ, Scotland, UK. swang@cyclacel.com
authors.forename: Shudong
authors.initials: S
authors.lastname: Wang
authors.forename: Gavin
authors.initials: G
authors.lastname: Wood
authors.forename: Christopher
authors.initials: C
authors.lastname: Meades
authors.forename: Gary
authors.initials: G
authors.lastname: Griffiths
authors.forename: Carol
authors.initials: C
authors.lastname: Midgley
authors.forename: Iain
authors.initials: I
authors.lastname: McNae
authors.forename: Campbell
authors.initials: C
authors.lastname: McInnes
authors.forename: Sian
authors.initials: S
authors.lastname: Anderson
authors.forename: Wayne
authors.initials: W
authors.lastname: Jackson
authors.forename: Mokdad
authors.initials: M
authors.lastname: Mezna
authors.forename: Rhoda
authors.initials: R
authors.lastname: Yuill
authors.forename: Malcolm
authors.initials: M
authors.lastname: Walkinshaw
authors.forename: Peter M
authors.initials: PM
authors.lastname: Fischer
mesh_terms: D045744:Cell Line, Tumor; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: C496609:2-anilino-4-(1H-pyrrol-3-yl) pyrimidine; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D011758:Pyrroles; D018844:Cyclin-Dependent Kinases