Literature DB >> 22326394

Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.

Adel S El-Azab1, Kamal E H Eltahir.   

Abstract

A novel series of 7-substituted-4(3H)-quinazolinone were designed, synthesized and evaluated for their antitumor and anticonvulsant activity. Compound 7 revealed broad-spectrum antitumor effectiveness toward numerous cell lines that belong to different tumor subpanels, whereas compounds 9 and 18 possess selective activity toward leukemia cell lines. Additionally, compounds 3, 15, 16, 18, 19 and 20 showed advanced anticonvulsant activity as well as lower neurotoxicity than reference drugs. The achieved results proved that the distinctive compounds could be valuable as a model for future devise, acclimatization and investigation to construct more active analogues.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22326394     DOI: 10.1016/j.bmcl.2012.01.071

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  12 in total

Review 1.  An insight into the therapeutic potential of quinazoline derivatives as anticancer agents.

Authors:  Irshad Ahmad
Journal:  Medchemcomm       Date:  2017-04-07       Impact factor: 3.597

2.  2-(2-{[4-Oxo-3-(2-phenyl-eth-yl)-3,4-dihydro-quinazolin-2-yl]sulfan-yl}eth-yl)-2,3-dihydro-1H-isoindole-1,3-dione.

Authors:  Adel S El-Azab; Alaa A-M Abdel-Aziz; Abdulrahman M Al-Obaid; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-13

3.  Synthesis, antitumour activities and molecular docking of thiocarboxylic acid ester-based NSAID scaffolds: COX-2 inhibition and mechanistic studies.

Authors:  Adel S El-Azab; Alaa A-M Abdel-Aziz; Laila A Abou-Zeid; Walaa M El-Husseiny; Ahmad M El Morsy; Manal A El-Gendy; Magda A-A El-Sayed
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

4.  Synthesis, in vitro antitumour activity, and molecular docking study of novel 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinone analogues.

Authors:  Adel S El-Azab; Alaa A-M Abdel-Aziz; Hazem A Ghabbour; Manal A Al-Gendy
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

5.  Methyl 3-[(6-nitro-4-oxo-3-phenyl-3,4-di-hydro-quinazolin-2-yl)sulfan-yl]propano-ate.

Authors:  Ibrahim A Al-Suwaidan; Alaa A-M Abdel-Aziz; Adel S El-Azab; C S Chidan Kumar; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-06-19

6.  2-Methyl-sulfanyl-9H-1,3,4-thia-diazolo[2,3-b]quinazolin-9-one.

Authors:  Adel S El-Azab; Alaa A-M Abdel-Aziz; Ibrahim A Al-Swaidan; Seik Weng Ng; Edward R T Tiekink
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-06-20

7.  Synthesis and biological evaluation of benzimidazole-linked 1,2,3-triazole congeners as agents.

Authors:  Karna Ji Harkala; Laxminarayana Eppakayala; Thirumala Chary Maringanti
Journal:  Org Med Chem Lett       Date:  2014-12-02

8.  Design and synthesis of chroman derivatives with dual anti-breast cancer and antiepileptic activities.

Authors:  Pinki Rawat; Saurabh Manaswita Verma
Journal:  Drug Des Devel Ther       Date:  2016-09-02       Impact factor: 4.162

9.  Synthesis, Anticancer Screening of Some Novel Trimethoxy Quinazolines and VEGFR2, EGFR Tyrosine Kinase Inhibitors Assay; Molecular Docking Studies.

Authors:  Abdulmalik S Altamimi; Adel S El-Azab; Sami G Abdelhamid; Mubarak A Alamri; Ashraf H Bayoumi; Safar M Alqahtani; Alhumaidi B Alabbas; Ali I Altharawi; Manal A Alossaimi; Menshawy A Mohamed
Journal:  Molecules       Date:  2021-05-18       Impact factor: 4.411

10.  Application of Deep Eutectic Solvents in the Synthesis of Substituted 2-Mercaptoquinazolin-4(3H)-Ones: A Comparison of Selected Green Chemistry Methods.

Authors:  Mario Komar; Tatjana Gazivoda Kraljević; Igor Jerković; Maja Molnar
Journal:  Molecules       Date:  2022-01-16       Impact factor: 4.411

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