Literature DB >> 20850308

Synthesis of novel pyrrole and pyrrolo[2,3-d]pyrimidine derivatives bearing sulfonamide moiety for evaluation as anticancer and radiosensitizing agents.

Mostafa M Ghorab1, Fatma A Ragab, Helmy I Heiba, Hanan A Youssef, Marwa G El-Gazzar.   

Abstract

Pyrroles and pyrrolo[2,3-d]pyrimidines were reported to act as potent anticancer agents, in this work, a series of novel 2-substituted-3-cyano-4-phenyl-pyrrole 5, 6, 11-18, and 5-phenyl-pyrrolo[2,3-d]pyrimidine derivatives 7-10, 19-24 bearing either sulfathiazole or sulfapyridine were synthesized. The structures of these compounds were confirmed by elemental analysis, IR, (1)H NMR and mass spectral data. All the newly synthesized compounds were evaluated for their in vitro cytotoxicity against liver and breast cancer cell line (HEPG2 and MCF7). Most of the screened compounds showed interesting cytotoxic activities compared with the used reference drug (doxorubicin). The radiosensitizing ability of some of the synthesized compounds was studied and the results showed an increase in the cell killing effect of γ-radiation after combination with the tested compounds.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20850308     DOI: 10.1016/j.bmcl.2010.08.005

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


  9 in total

1.  Novel Anticancer Fused Pyrazole Derivatives as EGFR and VEGFR-2 Dual TK Inhibitors.

Authors:  Nashwa M Saleh; Marwa G El-Gazzar; Hala M Aly; Rana A Othman
Journal:  Front Chem       Date:  2020-01-24       Impact factor: 5.221

2.  Exploring natural product chemistry and biology with multicomponent reactions. 5. Discovery of a novel tubulin-targeting scaffold derived from the rigidin family of marine alkaloids.

Authors:  Liliya V Frolova; Igor V Magedov; Anntherese E Romero; Menuka Karki; Isaiah Otero; Kathryn Hayden; Nikolai M Evdokimov; Laetitia Moreno Y Banuls; Shiva K Rastogi; W Ross Smith; Shi-Long Lu; Robert Kiss; Charles B Shuster; Ernest Hamel; Tania Betancourt; Snezna Rogelj; Alexander Kornienko
Journal:  J Med Chem       Date:  2013-08-23       Impact factor: 7.446

3.  Green and four-component cyclocondensation synthesis and in silico docking of new polyfunctionalized pyrrole derivatives as the potential anticholinesterase agents.

Authors:  Mohammad Hadi Meshkatalsadat; Ahmad Mahmoudi; Safa Lotfi; Behjat Pouramiri; Alireza Foroumadi
Journal:  Mol Divers       Date:  2022-01-16       Impact factor: 2.943

4.  Synthesis, characterization and anti-breast cancer activity of new 4-aminoantipyrine-based heterocycles.

Authors:  Mostafa M Ghorab; Marwa G El-Gazzar; Mansour S Alsaid
Journal:  Int J Mol Sci       Date:  2014-05-02       Impact factor: 5.923

5.  Absolute configuration of (1S,2S)-3-methyl-2-phenyl-2,3-dihydro-thia-zolo[2,3-b]quinazolin-5-one.

Authors:  Mostafa M Ghorab; Mansour S Al-Said; Maged S Abdel-Kader; Madhukar Hemamalini; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-03-03

6.  6-Chloro-2-chloro-methyl-4-phenyl-quinazoline 3-oxide.

Authors:  Thammarse S Yamuna; Jerry P Jasinski; Manpreet Kaur; Hemmige S Yathirajan; Maravanahalli S Siddegowda
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-03-15

7.  Synthesis and evaluation of novel pyrroles and pyrrolopyrimidines as anti-hyperglycemic agents.

Authors:  M S Mohamed; S A Ali; D H A Abdelaziz; Samar S Fathallah
Journal:  Biomed Res Int       Date:  2014-06-26       Impact factor: 3.411

8.  Synthesis of Some Benzofuran Derivatives Containing Pyrimidine Moiety as Potent Antimicrobial Agents.

Authors:  Talavara Venkatesh; Yadav Dasharathrao Bodke; Muthipeedika Nibin Joy; Bhadrapura Lakkappa Dhananjaya; Sivaramakrishnan Venkataraman
Journal:  Iran J Pharm Res       Date:  2018       Impact factor: 1.696

9.  Carbonic anhydrase inhibition with a series of novel benzenesulfonamide-triazole conjugates.

Authors:  Marwa G El-Gazzar; Nessma H Nafie; Alessio Nocentini; Mostafa M Ghorab; Helmi I Heiba; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2018-12       Impact factor: 5.051

  9 in total

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