Bioorganic and Medicinal Chemistry Letters p. 1973 - 1977 (2005)
Update date:2022-08-04
Topics:
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
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 (IC50 < 10 nM). 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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