Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors
Sharad Verma1, Dhanapalan Nagarathnam, Jianxing Shao
1Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. sharad.verma.b@bayer.com <sharad.verma.b@bayer.com>
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.
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