The first peptide derivatives of dioxybiphenyl-bridged spiro cyclotriphosphazenes: In vitro cytotoxicity activities and DNA damage studies

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dc.authoridTekin, Suat/0000-0002-2757-1802
dc.authoridKORAN, KENAN/0000-0002-2218-7211
dc.authoridSandal, Suleyman/0000-0002-8916-3329
dc.authoridGORGULU, AHMET/0000-0002-7549-1524
dc.authoridCAPAN, IRFAN/0000-0002-9555-1555
dc.authoridGorgulu, Ahmet Orhan/0000-0003-0632-4834
dc.authorwosidTekin, Suat/KEI-2266-2024
dc.authorwosidÇALIŞKAN, ERAY/W-6973-2018
dc.authorwosidKORAN, KENAN/L-6764-2016
dc.authorwosidSandal, Suleyman/AAA-6388-2021
dc.authorwosidGORGULU, AHMET/KBA-2787-2024
dc.authorwosidCAPAN, IRFAN/AAE-4102-2022
dc.contributor.authorKoran, Kenan
dc.contributor.authorCaliskan, Eray
dc.contributor.authorOzturk, Dilara Altay
dc.contributor.authorCapan, Irfan
dc.contributor.authorTekin, Suat
dc.contributor.authorSandal, Suleyman
dc.contributor.authorGorgulu, Ahmet Orhan
dc.date.accessioned2024-08-04T20:53:21Z
dc.date.available2024-08-04T20:53:21Z
dc.date.issued2023
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn this study, we aimed to synthesize new peptide-substituted cyclotriphosphazenes from a series of tyrosine -based peptides and dioxyphenyl-substituted spirocyclotriphosphazenes, and to evaluate their in vitro cytotox-icity and genotoxicity activities. Genotoxicity studies were conducted to understand whether the cytotoxic compounds cause cell death through DNA damage. The structures of the novel series of phosphazenes were characterized by FT-IR, elemental analysis, MS, 1D (31P, 1H, and 13C-APT NMR), and 2D (HETCOR) NMR spectroscopic techniques. In vitro cytotoxic activities were carried out against human breast (MCF-7), ovarian (A2780), prostate (PC-3), colon (Caco-2) cancer cell lines and human normal epithelial cell line (MCF-10A) at different concentrations by using an MTT assay. The compounds showed considerable reductions in cell viability against all human cancer cell lines. Especially, the compounds exhibited notable effects in A2780 cell lines (p < 0.05). The IC50 values of the compounds in the A2780 cell line were calculated to be 1.914 mu M for TG, 20.21 mu M for TV, 20.45 mu M for TA, 4.643 mu M for TP, 5.615 mu M for BTG, 1.047 mu M for BTV, 27.02 mu M for BTA, 0.7734 mu M for BTP, 21.5 mu M for DTG, 1.65 mu M for DTV, 2.89 mu M for DTA and 4.599 mu M for DTP. DNA damage studies of the compounds were conducted by the comet assay method using tail length, tail density, olive tail moment, head length, and head density parameters, and the results showed that the cell death occurred through DNA damage mechanism. In a nutshell, these compounds show promising cytotoxic effects and can be considered powerful candidate molecules for pharmaceutical applications.en_US
dc.description.sponsorshipScientific and Technical Research Council of Tuerkiye (TUBITAK) [118Z286]en_US
dc.description.sponsorshipThis work was supported by a grant from the Scientific and Technical Research Council of Tuerkiye (TUBITAK, Grant Number:118Z286). We would like to thank TUBITAK for their contributionen_US
dc.identifier.doi10.1016/j.bioorg.2022.106338
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid36603512en_US
dc.identifier.scopus2-s2.0-85145857915en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2022.106338
dc.identifier.urihttps://hdl.handle.net/11616/101101
dc.identifier.volume132en_US
dc.identifier.wosWOS:000918666200001en_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.subjectDNA damageen_US
dc.subjectPhosphazeneen_US
dc.subjectDipeptideen_US
dc.subjectCytotoxicityen_US
dc.titleThe first peptide derivatives of dioxybiphenyl-bridged spiro cyclotriphosphazenes: In vitro cytotoxicity activities and DNA damage studiesen_US
dc.typeArticleen_US

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