Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents

Samir M. EL-MOGHAZY; Diaa A. IBRAHIM; Nagwa M. ABDELGAWAD; Nahla A. H. FARAG; Ahmad S. EL-KHOULY

doi:10.3797/scipharm.1103-16

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Article

8 May 2011

Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents

and

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt

Department of Organic Chemistry, National Organization for Drug Control and Research, P.O. Box 29, Cairo, Giza 12311, Egypt

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University, Km 28 Cairo-Ismailia Road, Cairo, Egypt

Author to whom correspondence should be addressed.

Sci. Pharm.2011, 79(3), 429-448;https://doi.org/10.3797/scipharm.1103-16

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Abstract

A series of 2,5,7-trisubstituted pyrimido[4,5-d]pyrimidine cyclin-dependent kinase (CDK2) inhibitors is designed and synthesized. 6-Amino-2-thiouracil is reacted with an aldehyde and thiourea to prepare the pyrimido[4,5-d]-pyrimidines. Alkylation and amination of the latter ones give different amino derivatives. These compounds show potent and selective CDK inhibitory activities and inhibit in vitro cellular proliferation in cultured human tumor cells.

Keywords:

Drug Design; Pharmacophore; Pyrimido[4,5-d]pyrimidine; CDK2; Anti-tumor

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