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

Authors :
Bayomi, Said M.
El-Kashef, Hassan A.
El-Ashmawy, Mahmoud B.
Nasr, Magda N.A.
El-Sherbeny, Magda A.
Abdel-Aziz, Naglaa I.
El-Sayed, Magda A.-A.
Suddek, Ghada M.
El-Messery, Shahenda M.
Ghaly, Mariam A.
Source :
European Journal of Medicinal Chemistry. Aug2015, Vol. 101, p584-594. 11p.
Publication Year :
2015

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-2 H -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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
101
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
108943358
Full Text :
https://doi.org/10.1016/j.ejmech.2015.07.014