Synthesis, Biological Evaluation and Molecular Docking Studies of Bis-Chalcone Derivatives as Xanthine Oxidase Inhibitors and Anticancer Agents

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Date

2019

Authors

Burmaoğlu, Serdar
Özcan, Şeyda
Balcıoğlu, Sevgi
Gencel, Melis
Noma, Samir Abbas Ali
Eşsiz, Şebnem
Ateş, Burhan
Algül, Öztekin

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Elsevier

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Abstract

In this study, a series of B-ring fluoro substituted bis-chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and evaluated for their ability to inhibit xanthine oxidase (XO) and growth inhibitory activity against MCF-7 and Caco-2 human cancer cell lines, in vitro. According to the results obtained, the bis-chalcone with fluoro group at the 2 (4b) or 2,5-position (4g) of B-ring were found to be potent inhibitors of the enzyme with IC50 values in the low micromolar range. The effects of these compounds were about 7 fold higher than allopurinol. The binding modes of the bis-chalcone derivatives in the active site of xanthine oxidase were explained using molecular docking calculations. Also, compound 4g and 4h showed in vitro growth inhibitory activity against a panel of two human cancer cell lines 1.9 and 6.8 μM of IC50 values, respectively.

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Bis-chalcone, Claisen-Schmidt condensation, Cytotoxicity, Inhibition, Synthesis

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42

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Volume

91

Issue

10/01/19

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