title: Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors.
abstract: A series of aminobenzimidazole-substituted pyrimidines were synthesized and evaluated for biochemical activity against CDK1. A high-speed parallel synthesis approach enabled the identification of a potent lead series having improved potency in the CDK1 assay (IC(50)<10nM). Cell cycle analysis showed that the compounds induced a G2/M block. Docking studies were carried out with a CDK1 homology model, and provide a rationale for the observed activities.
authors.affiliation: Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. sharad.verma.b@bayer.com <sharad.verma.b@bayer.com>
authors.forename: Sharad
authors.initials: S
authors.lastname: Verma
authors.forename: Dhanapalan
authors.initials: D
authors.lastname: Nagarathnam
authors.forename: Jianxing
authors.initials: J
authors.lastname: Shao
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Jin
authors.initials: J
authors.lastname: Zhao
authors.forename: Yamin
authors.initials: Y
authors.lastname: Wang
authors.forename: Tindy
authors.initials: T
authors.lastname: Li
authors.forename: Eric
authors.initials: E
authors.lastname: Mull
authors.forename: Istvan
authors.initials: I
authors.lastname: Enyedy
authors.forename: Chunguang
authors.initials: C
authors.lastname: Wang
authors.forename: Qingming
authors.initials: Q
authors.lastname: Zhu
authors.forename: Martha
authors.initials: M
authors.lastname: Altieri
authors.forename: Jerold
authors.initials: J
authors.lastname: Jordan
authors.forename: Thu-Thi-Anh
authors.initials: TT
authors.lastname: Dang
authors.forename: Sanjeeva
authors.initials: S
authors.lastname: Reddy
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D018844:Cyclin-Dependent Kinases