4.7 Article

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

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 101, 期 -, 页码 584-594

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.07.014

关键词

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

资金

  1. Mansoura University research center, Egypt

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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-Chloropheny1)-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. (C) 2015 Elsevier Masson SAS. All rights reserved.

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