title: Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.
abstract: High-throughput screening identified the imidazo[1,2-a]pyridine and bisanilinopyrimidine series as inhibitors of the cyclin-dependent kinase CDK4. Comparison of their experimentally-determined binding modes and emerging structure-activity trends led to the development of potent and selective imidazo[1,2-a]pyridine inhibitors for CDK4 and in particular CDK2.
authors.affiliation: AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK.
authors.forename: Malcolm
authors.initials: M
authors.lastname: Anderson
authors.forename: John F
authors.initials: JF
authors.lastname: Beattie
authors.forename: Gloria A
authors.initials: GA
authors.lastname: Breault
authors.forename: Jason
authors.initials: J
authors.lastname: Breed
authors.forename: Kate F
authors.initials: KF
authors.lastname: Byth
authors.forename: Janet D
authors.initials: JD
authors.lastname: Culshaw
authors.forename: Rebecca P A
authors.initials: RP
authors.lastname: Ellston
authors.forename: Stephen
authors.initials: S
authors.lastname: Green
authors.forename: Claire A
authors.initials: CA
authors.lastname: Minshull
authors.forename: Richard A
authors.initials: RA
authors.lastname: Norman
authors.forename: Richard A
authors.initials: RA
authors.lastname: Pauptit
authors.forename: Judith
authors.initials: J
authors.lastname: Stanway
authors.forename: Andrew P
authors.initials: AP
authors.lastname: Thomas
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Jewsbury
mesh_terms: D042846:CDC2-CDC28 Kinases / Q000037:antagonists & inhibitors / Q000737:chemistry; D018360:Crystallography, X-Ray; D051357:Cyclin-Dependent Kinase 2; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011485:Protein Binding; D011518:Proto-Oncogene Proteins; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011518:Proto-Oncogene Proteins; D011725:Pyridines; D042846:CDC2-CDC28 Kinases; C495894:CDK2 protein, human; C495900:CDK4 protein, human; D051357:Cyclin-Dependent Kinase 2; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases