Literature DB >> 24763265

Design, synthesis and biological evaluation of some novel substituted quinazolines as antitumor agents.

Amer M Alanazi1, Alaa A-M Abdel-Aziz2, Ibrahim A Al-Suwaidan1, Sami G Abdel-Hamide3, Taghreed Z Shawer4, Adel S El-Azab5.   

Abstract

A novel series of 6-chloro-2-p-tolylquinazolinone and substituted-(4-methylbenzamido)benzamide (1-20) were designed, synthesized and evaluated for their in-vitro antitumor activity. Compounds 3, 14 and 16 possessed remarkable broad-spectrum antitumor activity. Compound 16 was found to be a particularly active growth inhibitor of the renal cancer (GI50 = 4.07 μM), CNS cancer (GI50 = 7.41 μM), ovarian cancer (GI50 = 7.41 μM) and non-small cell lung cancer (GI50 = 7.94 μM). Compound 16 ranks as nearly 1.5-fold more potent (mean GI50 = 15.8 μM) compared to 5-FU (mean GI50 = 22.6 μM).
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  In-vitro antitumor evaluation; NCI; Quinazoline; Selective activity; Synthesis

Mesh：

Substances：

Year:  2014        PMID： 24763265     DOI： 10.1016/j.ejmech.2014.04.029

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  12 in total

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

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2.  One-pot synthesis, biological evaluation and molecular docking studies of fused thiazolo[2,3-b]pyrimidinone-pyrazolylcoumarin hybrids.

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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.

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Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

8.  Synthesis, potential antitumor activity, cell cycle analysis, and multitarget mechanisms of novel hydrazones incorporating a 4-methylsulfonylbenzene scaffold: a molecular docking study.

Authors:  Alaa A-M Abdel-Aziz; Adel S El-Azab; Nawaf A AlSaif; Ahmad J Obaidullah; Abdulrahman M Al-Obaid; Ibrahim A Al-Suwaidan
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

9.  Synthesis, antitumour and antioxidant activities of novel α,β-unsaturated ketones and related heterocyclic analogues: EGFR inhibition and molecular modelling study.

Authors:  Walaa M El-Husseiny; Magda A-A El-Sayed; Naglaa I Abdel-Aziz; Adel S El-Azab; Esam R Ahmed; Alaa A-M Abdel-Aziz
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

10.  Synthesis, antitumor activity, and molecular docking study of 2-cyclopentyloxyanisole derivatives: mechanistic study of enzyme inhibition.

Authors:  Walaa M El-Husseiny; Magda A-A El-Sayed; Adel S El-Azab; Nawaf A AlSaif; Mohammed M Alanazi; Alaa A-M Abdel-Aziz
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
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