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Synthesis, biological evaluation and molecular docking studies of bis-chalcone derivatives as xanthine oxidase inhibitors and anticancer agents.

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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Burmaoglu S,Ozcan S,Balcioglu S,Gencel M,Noma SAA,Essiz S,Ates B,Algul O

doi

10.1016/j.bioorg.2019.103149

subject

Has Abstract

pub_date

2019-10-01 00:00:00

pages

103149

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)30350-5

journal_volume

91

pub_type

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