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

doi:10.1016/j.bmcl.2005.02.076

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 journal › Article › peer-review

21 Scopus citations

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 language	English (US)
Pages (from-to)	1973-1977
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2005.02.076
State	Published - Apr 15 2005
Externally published	Yes

ASJC Scopus subject areas

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

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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.",

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AU - Verma, Sharad

AU - Nagarathnam, Dhanapalan

AU - Shao, Jianxing

AU - Zhang, Lei

AU - Zhao, Jin

AU - Wang, Yamin

AU - Li, Tindy

AU - Mull, Eric

AU - Enyedy, Istvan

AU - Wang, Chunguang

AU - Zhu, Qingming

AU - Altieri, Martha

AU - Jordan, Jerold

AU - Dang, Thu Thi Anh

AU - Reddy, Sanjeeva

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AB - 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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JO - Bioorganic and Medicinal Chemistry Letters

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ER -

Substituted aminobenzimidazole pyrimidines as cyclin-dependent kinase inhibitors

Abstract

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