Assessing the Antiangiogenic Effects of Chalcones and Their Derivatives

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dc.authoridGUNER, ADEM/0000-0003-3295-3538
dc.authoridAKTAS ANIL, DERYA/0000-0003-2584-275X
dc.authoridKarabay Yavasoglu, N.Ulku/0000-0002-7483-0184
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.accessioned2025-03-23T19:35:08Z
dc.date.available2025-03-23T19:35:08Z
dc.date.issued2024
dc.departmentSinop Üniversitesi
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.
dc.identifier.doi10.1080/10406638.2023.2167216
dc.identifier.endpage66
dc.identifier.issn1040-6638
dc.identifier.issn1563-5333
dc.identifier.issue1
dc.identifier.scopus2-s2.0-85146993659
dc.identifier.scopusqualityQ2
dc.identifier.startpage51
dc.identifier.urihttps://doi.org/10.1080/10406638.2023.2167216
dc.identifier.urihttps://hdl.handle.net/11486/5789
dc.identifier.volume44
dc.identifier.wosWOS:000915991900001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherTaylor & Francis Ltd
dc.relation.ispartofPolycyclic Aromatic Compounds
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WOS_20250323
dc.subjectChalcone
dc.subjectanti-angiogenic activity
dc.subjectanti-proliferative activity
dc.subjectRT-qPCR
dc.subjectmolecular docking
dc.titleAssessing the Antiangiogenic Effects of Chalcones and Their Derivatives
dc.typeArticle

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