New Fluoro- and Trifluoromethyl-Substituted Trimethoxychalcones as Anticancer Agents: Synthesis, Bio-evaluation, and Computational Studies

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dc.authoridTURKMENOGLU, BURCIN/0000-0002-5770-0847
dc.contributor.authorPolat, M. Fatih
dc.contributor.authorAnil, Derya Aktas
dc.contributor.authorOzkemahli, Gizem
dc.contributor.authorTurkmenoglu, Burcin
dc.contributor.authorHepokur, Ceylan
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorAlgul, Oztekin
dc.date.accessioned2024-10-26T18:09:25Z
dc.date.available2024-10-26T18:09:25Z
dc.date.issued2023
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractWe designed and synthesized a novel series of trimethoxy chalcones with CF3 or F substituents at various positions of ring B, characterized using IR, NMR spectral data, and elemental analyses, based on the fact that methoxy and fluoro-substituted chalcones are included in the literature as a pharmacophore due to their anticancer activities. All compounds (12-21) were tested for cytotoxicity against A549, HEPG2, MCF7, and normal mouse fibroblasts (L929) using the XTT assay. The most active compound, 13, was also shown to induce MCF7 cell cycle arrest at the G0/G1 phase, indicating that they exert their antitumor potency via MCF7 cell apoptosis. The mechanisms involved in apoptotic cell death induced by compound 13 were also investigated to see if apoptotic proteins such as Bax, Bcl-2, and p53 were involved. In addition, the compounds with the strongest apoptotic effects against human EGFR and VEGFR-2 receptors were studied in silico. Finally, methoxy and fluoro-substituted chalcones derivatives have been shown to have potent anticancer properties.
dc.description.sponsorshipErzincan Binali Yildirim University Scientific Research Projects Coordination Commission [TSA-2020-705]; Erzincan Binali Yildirim University, Basic Sciences Application and Research Center (EBYU-EUTAM)
dc.description.sponsorshipThis study was supported by Erzincan Binali Yildirim University Scientific Research Projects Coordination Commission (Project No. TSA-2020-705). The authors would like to thank Erzincan Binali Yildirim University, Basic Sciences Application and Research Center (EBYU-EUTAM) for the Schroedinger Maestro 2021-2 program.
dc.identifier.doi10.1002/slct.202301189
dc.identifier.issn2365-6549
dc.identifier.issue32
dc.identifier.scopus2-s2.0-85168701427
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1002/slct.202301189
dc.identifier.urihttps://hdl.handle.net/20.500.12418/30083
dc.identifier.volume8
dc.identifier.wosWOS:001052692300001
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherWiley-V C H Verlag Gmbh
dc.relation.ispartofChemistryselect
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAnticancer activity
dc.subjectchalcones
dc.subjectClaisen-Schmidt condensation
dc.subjectmolecular docking
dc.subjectSynthesis
dc.titleNew Fluoro- and Trifluoromethyl-Substituted Trimethoxychalcones as Anticancer Agents: Synthesis, Bio-evaluation, and Computational Studies
dc.typeArticle

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