Next Article in Journal
Design, Synthesis and Biological Evaluation of New 5,5-Diarylhydantoin Derivatives as Selective Cyclooxygenase-2 Inhibitors
Previous Article in Journal
Neglected Disease – African Sleeping Sickness: Recent Synthetic and Modeling Advances
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
Sci. Pharm.
Volume 79
Issue 3
10.3797/scipharm.1103-16
scipharm-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles thumb_up
...
Endorse textsms
...
Comment
Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Article

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

by
Samir M. EL-MOGHAZY
1,
Diaa A. IBRAHIM
2,*,
Nagwa M. ABDELGAWAD
1,
Nahla A. H. FARAG
3 and
Ahmad S. EL-KHOULY
2
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.
Sci. Pharm. 2011, 79(3), 429-448; https://doi.org/10.3797/scipharm.1103-16
Submission received: 23 March 2011 / Accepted: 8 May 2011 / Published: 8 May 2011
Versions Notes

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

Share and Cite

MDPI and ACS Style

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. https://doi.org/10.3797/scipharm.1103-16

AMA Style

EL-MOGHAZY SM, IBRAHIM DA, ABDELGAWAD NM, FARAG NAH, EL-KHOULY AS. Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents. Scientia Pharmaceutica. 2011; 79(3):429-448. https://doi.org/10.3797/scipharm.1103-16

Chicago/Turabian Style

EL-MOGHAZY, Samir M., Diaa A. IBRAHIM, Nagwa M. ABDELGAWAD, Nahla A. H. FARAG, and Ahmad S. EL-KHOULY. 2011. "Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents" Scientia Pharmaceutica 79, no. 3: 429-448. https://doi.org/10.3797/scipharm.1103-16

APA Style

EL-MOGHAZY, S. M., IBRAHIM, D. A., ABDELGAWAD, N. M., FARAG, N. A. H., & EL-KHOULY, A. S. (2011). Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents. Scientia Pharmaceutica, 79(3), 429-448. https://doi.org/10.3797/scipharm.1103-16

Article Metrics

Back to TopTop