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

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dc.authoridALGUL, OZTEKIN/0000-0001-5685-7511
dc.authoridAteş, Burhan/0000-0001-6080-229X
dc.authoridBALCIOGLU, Sevgi/0000-0003-0724-4772
dc.authoridBALCIOGLU, Sevgi/0000-0003-0724-4772
dc.authoridEssiz, Sebnem/0000-0002-5476-4722
dc.authorwosidALGUL, OZTEKIN/N-3043-2019
dc.authorwosidAteş, Burhan/AAA-3730-2021
dc.authorwosidBALCIOGLU, Sevgi/W-5874-2018
dc.authorwosidBALCIOGLU, Sevgi/O-3576-2015
dc.authorwosidNOMA, SAMIR/ABH-1773-2021
dc.authorwosidEssiz, Sebnem/JVZ-2123-2024
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorOzcan, Seyda
dc.contributor.authorBalcioglu, Sevgi
dc.contributor.authorGencel, Melis
dc.contributor.authorNoma, Samir Abbas Ali
dc.contributor.authorEssiz, Sebnem
dc.contributor.authorAtes, Burhan
dc.date.accessioned2024-08-04T20:46:46Z
dc.date.available2024-08-04T20:46:46Z
dc.date.issued2019
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn 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 mu M of IC50 values, respectively.en_US
dc.description.sponsorshipScientific and Technological Research Council of Turkey (TUBITAK) [114Z554]en_US
dc.description.sponsorshipWe thank the Scientific and Technological Research Council of Turkey (TUBITAK. Grant Number: 114Z554).en_US
dc.identifier.doi10.1016/j.bioorg.2019.103149
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid31382060en_US
dc.identifier.scopus2-s2.0-85071831143en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2019.103149
dc.identifier.urihttps://hdl.handle.net/11616/98945
dc.identifier.volume91en_US
dc.identifier.wosWOS:000487812000046en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.ispartofBioorganic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectBis-chalconeen_US
dc.subjectSynthesisen_US
dc.subjectClaisen-Schmidt condensationen_US
dc.subjectInhibitionen_US
dc.subjectCytotoxicityen_US
dc.titleSynthesis, biological evaluation and molecular docking studies of bis-chalcone derivatives as xanthine oxidase inhibitors and anticancer agentsen_US
dc.typeArticleen_US

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