Literature DB >> 26890117

Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds.

Menshawy A Mohamed1, Rezk R Ayyad2, Taghreed Z Shawer2, Alaa A-M Abdel-Aziz3, Adel S El-Azab4.   

Abstract

A novel series of 2-[(3-substituted-4(3H)-quinazolin-2-yl)thio]-N-(3,4,5-trimethoxyphenyl)acetamide (15-21) and 3-[(3-substituted-4(3H)-quinazolin-2-yl)thio])-N-(3,4,5-trimethoxyphenyl)propanamide (23-29) were designed, prepared and estimated for their anticancer activity in a solo dose 10 μM of the test compounds in the NCI 57 cell lines panel assay. Compounds 20, 23, 26, 27 and 28 revealed extensive-spectrum antitumor efficiency to numerous cell lines that belong to various tumor subpanels, while compounds 15, 16 and 19 possessed perceptive activity toward A498 and UO-31 renal cancer cell lines, and compound 17 showed selective effectiveness against NSC lung cancer NCI-H522 cell line. Additionally, compound 18 showed advanced activity against SR leukemia cell line, NSC lung cancer HOP-92 and renal cancer UO-31 cell lines.
Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anticancer; Broad spectrum; NCI; Quinazoline scaffolds; Synthesis

Mesh:

Substances:

Year:  2016        PMID: 26890117     DOI: 10.1016/j.ejmech.2016.02.002

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


  15 in total

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3.  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

4.  Synthesis and biological evaluation of 2-styrylquinolines as antitumour agents and EGFR kinase inhibitors: molecular docking study.

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

5.  Exploring structure-activity relationship of S-substituted 2-mercaptoquinazolin-4(3H)-one including 4-ethylbenzenesulfonamides as human carbonic anhydrase inhibitors.

Authors:  Adel S El-Azab; Alaa A-M Abdel-Aziz; Hany E A Ahmed; Sivia Bua; Alessio Nocentini; Nawaf A AlSaif; Ahmad J Obaidullah; Mohamed M Hefnawy; Claudiu T Supuran
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Authors:  Alaa A-M Abdel-Aziz; Adel S El-Azab; Nawaf A AlSaif; Mohammed M Alanazi; Manal A El-Gendy; Ahmad J Obaidullah; Hamad M Alkahtani; Abdulrahman A Almehizia; Ibrahim A Al-Suwaidan
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

7.  Synthesis, Antiproliferative, and Antioxidant Evaluation of 2-Pentylquinazolin-4(3H)-one(thione) Derivatives with DFT Study.

Authors:  Amira A El-Sayed; Mahmoud F Ismail; Abd El-Galil E Amr; Ahmed M Naglah
Journal:  Molecules       Date:  2019-10-21       Impact factor: 4.411

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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