Assessing the Antiangiogenic Effects of Chalcones and Their Derivatives

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dc.authoridAnıl, Derya Aktas/0000-0003-2584-275X
dc.authoridYavasoglu, N.Ulku Karabay/0000-0002-7483-0184
dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authoridGUNER, ADEM/0000-0003-3295-3538
dc.authorwosidAnıl, Derya Aktas/GVU-7548-2022
dc.authorwosidYavasoglu, N.Ulku Karabay/AFU-9719-2022
dc.authorwosidAktas Anıl, Derya/AAA-3525-2022
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorGobek, Arzu
dc.contributor.authorAnil, Derya Aktas
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorGuner, Adem
dc.contributor.authorGuler, Cem
dc.contributor.authorHepokur, Ceylan
dc.date.accessioned2024-08-04T20:53:22Z
dc.date.available2024-08-04T20:53:22Z
dc.date.issued2024
dc.departmentİnönü Üniversitesien_US
dc.description.abstractPathological angiogenesis plays a critical role in tumorigenesis and tumor progression, and anti-angiogenesis therapies have evinced promising antitumor effects in solid tumors. Chalcone skeleton has been regarded as a potential antitumor agent that also targets angiogenesis. In this study, we designed twenty-one non-fluoro-substituted chalcones (13-18, 24-27) and saturated chalcone derivatives (19-23, 28-33) as anti-angiogenic compounds. During the initial stage, these compounds were assessed for their anti-cancer activities against MCF-7 cancer cell lines according to the MTT assay. The compounds revealed satisfactory anti-proliferative capability. An ex vivo fertilized hens' egg-chorioallantoic membrane (HET-CAM) angiogenic study was conducted for the compounds to gauge their mortality and toxicity, which, in turn, revealed a potent anti-angiogenic effect. Eight compounds (16, 17, 21, 24, 26, 27, 29, and 31) significantly reduced densities of capillaries on CAM, whereas compounds 27 and 29 were the most effective anti-angiogenic agents, when compared with Suramin. Moreover, RT-qPCR analysis demonstrated that the anti-angiogenic activity was associated with the fold changes of VEGFR2. Molecular docking studies were conducted for compounds to investigate their mode of interaction within the binding site of VEGFR-2 kinases. This work provided a basis for further design, structural modification, and development of chalcone derivatives as new anti-angiogenic agents.en_US
dc.identifier.doi10.1080/10406638.2023.2167216
dc.identifier.endpage66en_US
dc.identifier.issn1040-6638
dc.identifier.issn1563-5333
dc.identifier.issue1en_US
dc.identifier.scopus2-s2.0-85146993659en_US
dc.identifier.scopusqualityQ3en_US
dc.identifier.startpage51en_US
dc.identifier.urihttps://doi.org/10.1080/10406638.2023.2167216
dc.identifier.urihttps://hdl.handle.net/11616/101138
dc.identifier.volume44en_US
dc.identifier.wosWOS:000915991900001en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofPolycyclic Aromatic Compoundsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectChalconeen_US
dc.subjectanti-angiogenic activityen_US
dc.subjectanti-proliferative activityen_US
dc.subjectRT-qPCRen_US
dc.subjectmolecular dockingen_US
dc.titleAssessing the Antiangiogenic Effects of Chalcones and Their Derivativesen_US
dc.typeArticleen_US

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