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oai:ebyu-rdlopen.rawdatalibrary.net:ebyu/115622026-10-18T20:26:35Zopenairedrivercom_ebyu_10000col_ebyu_10001

Assessing the Antiangiogenic Effects of Chalcones and Their DerivativesBurmaoglu, SerdarGobek, ArzuAnil, Derya AktasAlagoz, Mehmet AbdullahGuner, AdemGüler, CemHepokur, CeylanKarabay Yavasoglu, N. UlkuAlgul, Oztekinanti-angiogenic activityanti-proliferative activityChalconemolecular dockingRT-qPCRBinding sitesCamsCell cultureDiseasesMolecular modelingTumorsAngiogenesisAntiangiogenicAntiproliferative activitiesChalcone derivativesChalconesTumor progressionsTumorigenesisPolymerase chain reactionPathological 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. © 2023 Taylor & Francis Group, LLC.Taylor and Francis Ltd.2024Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/11562https://doi.org/10.1080/10406638.2023.21672161040-6638enPolycyclic Aromatic Compoundsinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/11562