Author/Authors :
Sharad Verma، نويسنده , , Dhanapalan Nagarathnam، نويسنده , , Jianxing Shao، نويسنده , , Lei Zhang، نويسنده , , Jin Zhao، نويسنده , , Yamin Wang، نويسنده , , Tindy Li، نويسنده , , Eric Mull، نويسنده , , Istvan Enyedy، نويسنده , , Chunguang Wang، نويسنده , , Qingming Zhu، نويسنده , , Martha Altieri، نويسنده , , Jerold Jordan، نويسنده , , Thu-Thi-Anh Dang، نويسنده , , Sanjeeva Reddy، نويسنده ,
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 (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.
