Hexa-substituted cyclotriphosphazene derivatives containing hetero-ring chalcones: Synthesis, in vitro cytotoxic activity and their DNA damage determination

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dc.authoridSandal, Suleyman/0000-0002-8916-3329
dc.authoridTekin, Suat/0000-0002-2757-1802
dc.authoridGORGULU, AHMET/0000-0002-7549-1524
dc.authoridKORAN, KENAN/0000-0002-2218-7211
dc.authoridGorgulu, Ahmet Orhan/0000-0003-0632-4834
dc.authorwosidSandal, Suleyman/AAA-6388-2021
dc.authorwosidTekin, Suat/KEI-2266-2024
dc.authorwosidÇALIŞKAN, ERAY/W-6973-2018
dc.authorwosidGORGULU, AHMET/KBA-2787-2024
dc.authorwosidKORAN, KENAN/L-6764-2016
dc.contributor.authorBeytur, Asiye
dc.contributor.authorTekin, Cigdem
dc.contributor.authorCaliskan, Eray
dc.contributor.authorTekin, Suat
dc.contributor.authorKoran, Kenan
dc.contributor.authorGorgulu, Ahmet Orhan
dc.contributor.authorSandal, Suleyman
dc.date.accessioned2024-08-04T20:52:06Z
dc.date.available2024-08-04T20:52:06Z
dc.date.issued2022
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn this study, hetero ring hexasubstituted cyclotriphosphazes were obtained in two steps and these compounds were investigated in terms of in vitro cytotoxicity and genotoxicity. The structural characterizations of the starting compounds 1-4 were defined by FT-IR, elemental analysis, and NMR (1H and 13C) spectroscopy techniques. In addition to these techniques, the 31P NMR spectroscopy technique was also used in the characterization of cyclotriphosphazenes (FSC 1-4). The changes in cell viability at 1, 5, 25, 50, and 100 mu M concentrations against human ovarian (A2780) and human prostate (PC-3 and LNCaP) cell lines for 24 h were determined by the MTT assay method. According to MTT assay results, the inhibitory concentration 50 (IC50/ LogIC50) value was calculated in Graphpad Prism 6 program. The comet assay was performed to determine whether the effects of compounds on cell viability were through DNA damage. In the comet assay experiments, the highest concentration of compounds (100 mu M) was applied to the cells for 24 h and tail length (TL), tail intensity (TI), olive tail moment (OTM) parameters were examined. The results showed that the compound 1-4 and FSC 1-4 compounds reduced the cell viability against all cancer cell lines (p < 0.05). At the same time, different concentrations of these compounds caused DNA damage in all three cell types (p < 0.05). The possible interactions and chemical mechanisms of the synthesized compounds were explained by computational methods with molecular docking. In addition, pharmacological properties of drug candidate molecules have been defined. Experimental and calculated data comply with each other. The study results showed that these compounds have cytotoxic effects against cancer cells and suggested that these effects have occurred through genotoxicity.en_US
dc.description.sponsorshipInonu University BAP [TCD-2017-675]en_US
dc.description.sponsorshipThis work was supported by Inonu University BAP (Grant number: TCD-2017-675) .en_US
dc.identifier.doi10.1016/j.bioorg.2022.105997
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid35792316en_US
dc.identifier.scopus2-s2.0-85133227762en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2022.105997
dc.identifier.urihttps://hdl.handle.net/11616/100759
dc.identifier.volume127en_US
dc.identifier.wosWOS:000826737200002en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.ispartofBioorganic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectCyclotriphosphazeneen_US
dc.subjectCytotoxicityen_US
dc.subjectGenotoxicityen_US
dc.subjectChalconesen_US
dc.subjectSynthesisen_US
dc.titleHexa-substituted cyclotriphosphazene derivatives containing hetero-ring chalcones: Synthesis, in vitro cytotoxic activity and their DNA damage determinationen_US
dc.typeArticleen_US

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