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Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors |
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| Authors: | Verma Sharad Nagarathnam Dhanapalan Shao Jianxing Zhang Lei Zhao Jin Wang Yamin Li Tindy Mull Eric Enyedy Istvan Wang Chunguang Zhu Qingming Altieri Martha Jordan Jerold Dang Thu-Thi-Anh Reddy Sanjeeva |
| Institution: | Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. 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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