Literature DB >> 21886895

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

Samir M El-Moghazy1, Diaa A Ibrahim, Nagwa M Abdelgawad, Nahla A H Farag, Ahmad S El-Khouly.   

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.

Entities:  

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

Year:  2011        PMID： 21886895      PMCID： PMC3163380          DOI： 10.3797/scipharm.1103-16

Source DB:  PubMed          Journal:  Sci Pharm        ISSN： 0036-8709


  20 in total

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Journal:  Nat Rev Mol Cell Biol       Date:  2001-01       Impact factor: 94.444

2.  Antitumor and antiviral activity of synthetic alpha- and beta-ribonucleosides of certain substituted pyrimido[5,4-d]pyrimidines: a new synthetic strategy for exocyclic aminonucleosides.

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3.  1,4-dioxane-fused 4-anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase.

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Journal:  Arch Pharm (Weinheim)       Date:  2001-11       Impact factor: 3.751

4.  A convenient synthesis and hepatoprotective activity of imidazo[1,2-c]pyrimido[5,4-e]pyrimidine, tetraazaacenaphthene and tetraazaphenalene from cyclic ketene aminals through tandem addition-cyclization reactions.

Authors:  Vishnu J Ram; Atul Goel; Sanjay Sarkhel; Prakas R Maulik
Journal:  Bioorg Med Chem       Date:  2002-05       Impact factor: 3.641

5.  Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.

Authors:  G W Rewcastle; A J Bridges; D W Fry; J R Rubin; W A Denny
Journal:  J Med Chem       Date:  1997-06-06       Impact factor: 7.446

6.  Inhibition of herpes simplex virus reactivation by dipyridamole.

Authors:  R B Tenser; A Gaydos; K A Hay
Journal:  Antimicrob Agents Chemother       Date:  2001-12       Impact factor: 5.191

7.  New colorimetric cytotoxicity assay for anticancer-drug screening.

Authors:  P Skehan; R Storeng; D Scudiero; A Monks; J McMahon; D Vistica; J T Warren; H Bokesch; S Kenney; M R Boyd
Journal:  J Natl Cancer Inst       Date:  1990-07-04       Impact factor: 13.506

8.  Synthesis of quaternised 2-aminopyrimido[4,5-d]pyrimidin-4(3H)-ones and their biological activity with dihydrofolate reductase.

Authors:  Markus G Gebauer; Carolyn McKinlay; Jill E Gready
Journal:  Eur J Med Chem       Date:  2003 Jul-Aug       Impact factor: 6.514

9.  1-(2-Nitro-phen-yl)-3-phenyl-thio-urea.

Authors:  Yongqi Qin; Fangfang Jian; Mingna Jiang; Xiangyan Yang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2007-12-06

10.  Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents.

Authors:  D A Ibrahim
Journal:  Eur J Med Chem       Date:  2009-01-19       Impact factor: 6.514
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  4 in total

1.  Preparation of tetrasubstituted pyrimido[4,5-d]pyrimidine diones.

Authors:  Hui Wang; Chao Wang; Thomas D Bannister
Journal:  Tetrahedron Lett       Date:  2015-04-08       Impact factor: 2.415

Review 2.  A Review on Fused Pyrimidine Systems as EGFR Inhibitors and Their Structure-Activity Relationship.

Authors:  Tanuja T Yadav; Gulam Moin Shaikh; Maushmi S Kumar; Meena Chintamaneni; Mayur Yc
Journal:  Front Chem       Date:  2022-06-13       Impact factor: 5.545

Review 3.  Advances in the chemical and biological diversity of heterocyclic systems incorporating pyrimido[1,6-a]pyrimidine and pyrimido[1,6-c]pyrimidine scaffolds.

Authors:  Khaled M Elattar; Başak Doğru Mert; M Monier; Ahmed El-Mekabaty
Journal:  RSC Adv       Date:  2020-04-20       Impact factor: 4.036

4.  TBHP-mediated oxidative synthesis of substituted pyrimido[4,5-d]pyrimidines from N-uracil amidines and methylarenes under metal free conditions.

Authors:  Pradip Debnath
Journal:  RSC Adv       Date:  2019-09-20       Impact factor: 4.036
  4 in total

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