Design, synthesis and biological evaluation of novel bischalcone derivatives as potential anticancer agents

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dc.authoridozturk aydin, busra/0000-0002-0045-5254
dc.authoridYalcin, Gozde/0000-0002-9689-2239
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorGobek, Arzu
dc.contributor.authorAydin, Busra Ozturk
dc.contributor.authorYurtoglu, Emine
dc.contributor.authorAydin, Busra Nur
dc.contributor.authorOzkat, Gozde Yalcin
dc.contributor.authorHepokur, Ceylan
dc.date.accessioned2024-10-26T18:10:49Z
dc.date.available2024-10-26T18:10:49Z
dc.date.issued2021
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractBuilding on our previous work that discovered chalcone as a promising pharmacophore for anticancer activity, we have various other chalcone derivatives and have synthesized a series of novel bischalcone to explore their anticancer activity. Among all tested compounds, compounds 6a, 6b, and 6c showed the highest antiproliferative activity against A-549 cancer cell lines with the average IC50 values of 4.18, 4.52, and 5.05 & micro;M, respectively. Moreover, compound 6c showed high antiproliferative activity against the Caco-2 cell line; thus, it was 2- and 4fold more active than the reference compounds, i.e., methotrexate and capecitabine. Compound 6a also induced cell-cycle arrest in the S phase, whereas compounds 6b and 6c were observed to stop at the G0/G1 phase. Thereafter, we evaluated that compound 6c also had the highest apoptosis/necrosis ratio than other compounds and the standard compound. The anticancer property of the 6c was also supported by molecular docking studies carried out on the EGFR and HER2 receptors. Overall, we expect that these compounds can be further developed for the potential treatment of lung cancer.
dc.identifier.doi10.1016/j.bioorg.2021.104882
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid33839582
dc.identifier.scopus2-s2.0-85103754484
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2021.104882
dc.identifier.urihttps://hdl.handle.net/20.500.12418/30379
dc.identifier.volume111
dc.identifier.wosWOS:000656967400006
dc.identifier.wosqualityQ1
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherAcademic Press Inc Elsevier Science
dc.relation.ispartofBioorganic Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectBischalcone
dc.subjectSynthesis
dc.subjectMTT
dc.subjectFlow cytometry
dc.subjectCell cycle
dc.titleDesign, synthesis and biological evaluation of novel bischalcone derivatives as potential anticancer agents
dc.typeArticle

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