Medicinal Chemistry Research p. 1147 - 1162 (2013)
Update date:2022-07-29
Topics:
Bayomi, Said M.
El-Kashef, Hassan A.
El-Ashmawy, Mahmoud B.
Nasr, Magda N. A.
El-Sherbeny, Magda A.
Badria, Farid A.
Abou-Zeid, Laila A.
Ghaly, Mariam A.
Abdel-Aziz, Naglaa I.
Twenty-four new compounds were prepared, taking curcumin as a lead, in order to explore their antioxidant and antitumor properties. The capacities of these derivatives to scavenge the 2,2′-azinobis(3-ethylbenzothiazoline-6- sulfonic acid) radical cation (ABTS.+), and to protect human red blood cells (RBCs) from oxidative haemolysis were investigated. In addition, the percentage viability of different cell lines (Hep G2, WI38, VERO and MCF-7) was tested. The result of the antitumor testing was generally in accordance with those of the antioxidant assays. Compounds which bear o-methoxy substitution to the 4-hydroxy function in the phenyl ring (7g, 5g and 3g) exhibited significantly higher ABTS.+-scavenging, antihaemolysis, and antitumor activities than other derivatives. In addition, molecular modelling studies were carried out for biologically active and inactive compounds, to study the structure-activity relationship, with the aim to elucidate which portions of the molecules are critical for the antioxidant and antitumor activity.
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