Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors

Sharad Verma, Dhanapalan Nagarathnam, Jianxing Shao, Lei Zhang, Jin Zhao, Yamin Wang, Tindy Li, Eric Mull, Istvan Enyedy, Chunguang Wang, Qingming Zhu, Martha Altieri, Jerold Jordan, Thu Thi Anh Dang, Sanjeeva Reddy

Research output: Contribution to journalArticle

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.

Original languageEnglish (US)
Pages (from-to)1973-1977
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number8
DOIs
StatePublished - Apr 15 2005

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    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, T. T. A., & Reddy, S. (2005). Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 15(8), 1973-1977. https://doi.org/10.1016/j.bmcl.2005.02.076