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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
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Sci. Pharm. 2011, 79(3), 429-448; https://doi.org/10.3797/scipharm.1103-16 (registering DOI)

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

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt
2
Department of Organic Chemistry, National Organization for Drug Control and Research, P.O. Box 29, Cairo, Giza 12311, Egypt
3
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Misr International University, Km 28 Cairo-Ismailia Road, Cairo, Egypt
*
Author to whom correspondence should be addressed.
Received: 23 March 2011 / Accepted: 8 May 2011 / Published: 8 May 2011
PDF [583 KB, uploaded 28 September 2016]

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 Drug Design; Pharmacophore; Pyrimido[4,5-d]pyrimidine; CDK2; Anti-tumor
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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EL-MOGHAZY, S.M.; IBRAHIM, D.A.; ABDELGAWAD, N.M.; FARAG, N.A.H.; EL-KHOULY, A.S. Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents. Sci. Pharm. 2011, 79, 429-448.

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