Literature DB >> 26197162

Synthesis and biological evaluation of new curcumin analogues as antioxidant and antitumor agents: molecular modeling study.

Said M Bayomi1, Hassan A El-Kashef2, Mahmoud B El-Ashmawy1, Magda N A Nasr3, Magda A El-Sherbeny1, Naglaa I Abdel-Aziz1, Magda A-A El-Sayed3, Ghada M Suddek2, Shahenda M El-Messery3, Mariam A Ghaly4.   

Abstract

New curcumin analogues have been synthesized and their antioxidant activities were investigated by measuring their free radical scavenging capacities. The in vitro and in vivo antitumor activities of the synthesized compounds on Ehrlich ascites carcinoma (EAC) cell line were evaluated. 4-(4-Chlorophenyl)-2-(5-ethyl-7-(4-methoxybenzylidene)-3-(4-methoxyphenyl)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo[4,3-c] pyridin-2-yl)thiazole 7h showed excellent antineoplastic activity in both in vitro and in vivo studies more than that of tested compounds and reference drug, cisplatin. Different molecular modeling studies were performed, where docking of compound 7h into telomerase active site suggested that it could exert its antitumor potential by telomerase inhibition.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antioxidant effect; Antitumor effect; Curcumin analogues; Molecular modeling studies; Synthesis

Mesh:

Substances:

Year:  2015        PMID: 26197162     DOI: 10.1016/j.ejmech.2015.07.014

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


  4 in total

1.  Neuroprotective effects of curcumin against acetamiprid-induced neurotoxicity and oxidative stress in the developing male rat cerebellum: biochemical, histological, and behavioral changes.

Authors:  Ines Bini Dhouib; Alya Annabi; Raoudha Doghri; Ines Rejeb; Yosra Dallagi; Yassin Bdiri; Mohamed Montassar Lasram; Amel Elgaaied; Raja Marrakchi; Saloua Fazaa; Asma Gati
Journal:  Environ Sci Pollut Res Int       Date:  2017-10-04       Impact factor: 4.223

Review 2.  Bioactive Diarylpentanoids: Insights into the Biological Effects beyond Antitumor Activity and Structure-Activity Relationships.

Authors:  Joana Moreira; Lucilia Saraiva; Madalena M Pinto; Honorina Cidade
Journal:  Molecules       Date:  2022-09-26       Impact factor: 4.927

3.  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

4.  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

  4 in total

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