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.

journal_name

Bioorg Med Chem Lett

authors

Verma S,Nagarathnam D,Shao J,Zhang L,Zhao J,Wang Y,Li T,Mull E,Enyedy I,Wang C,Zhu Q,Altieri M,Jordan J,Dang TT,Reddy S

doi

10.1016/j.bmcl.2005.02.076

subject

Has Abstract

pub_date

2005-04-15 00:00:00

pages

1973-7

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00269-6

journal_volume

15

pub_type

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