Synthesis of naproxen thiadiazole urea hybrids and determination of their anti-melanoma, anti-migration, tyrosinase inhibitory activity, and molecular docking studies

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dc.authoridSönmez, Fatih/0000-0001-7486-6374
dc.authoridAkdemir, Atilla/0000-0001-8416-0471
dc.authoridOzturk Civelek, Dilek/0000-0003-2485-891X
dc.authoridKurt, Belma Zengin/0000-0002-4663-5402
dc.authoridGunaydin Akyildiz, Aysenur/0000-0003-1196-9530
dc.authoridçakmak, Ümmühan/0000-0001-8719-2436
dc.authoridGokce, Mustafa/0000-0003-4996-7370
dc.authorwosidSönmez, Fatih/AAR-5428-2020
dc.authorwosidAkdemir, Atilla/G-2595-2015
dc.authorwosidOzturk Civelek, Dilek/AAD-9249-2020
dc.authorwosidKurt, Belma Zengin/W-9070-2019
dc.authorwosidGunaydin Akyildiz, Aysenur/AAK-1806-2021
dc.authorwosidçakmak, Ümmühan/AAJ-7614-2021
dc.authorwosidGokce, Mustafa/N-7297-2018
dc.contributor.authorKurt, Belma Zengin
dc.contributor.authorAltundag, Ozlem
dc.contributor.authorGokce, Mustafa
dc.contributor.authorCakmak, Ummuhan
dc.contributor.authorTuncay, Fulya Oz
dc.contributor.authorKolcuoglu, Yakup
dc.contributor.authorAkyildiz, Aysenur Gunaydin
dc.date.accessioned2024-05-19T14:45:58Z
dc.date.available2024-05-19T14:45:58Z
dc.date.issued2024
dc.departmentİstinye Üniversitesien_US
dc.description.abstractNovel sixteen naproxen urea compounds were synthesized bearing the thiadiazole ring. Their inhibitory activities against tyrosinase were investigated. 3o was discovered to be the most potent inhibitor of tyrosinase, with an IC50 value of 35.0 mu M. The kinetic parameters were used to determine the type of enzyme inhibition. The results showed that 3o was an uncompetitive inhibitor with the Ki value of 62.2 mu M. Additionally, the cytotoxic effects of the synthesized compounds on melanoma (B16F10), mouse embryonic (3T3) and the healthy 3T3 cell lines were also investigated. According to the cytotoxicity results, 3e (IC50= 2.17 mu M) showed the highest cytotoxicity on the B16F10 cells. Furthermore, the effects of selected compounds on the migration rate of melanoma cells were investigated. In addition, molecular modeling studies were also performed and the results showed the possible interactions between the uncompetitive inhibitor 3o with the Tyrosinase-L-Tyrosine enzyme substrate complex.en_US
dc.description.sponsorshipBezmialem Research Fund of the Bezmialem Vakif University [12.2017/31]en_US
dc.description.sponsorshipThis work was supported by the Bezmialem Research Fund of the Bezmialem Vakif University. Project Number: 12.2017/31.en_US
dc.identifier.doi10.1016/j.molstruc.2023.136618
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85171343037en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org10.1016/j.molstruc.2023.136618
dc.identifier.urihttps://hdl.handle.net/20.500.12713/5405
dc.identifier.volume1295en_US
dc.identifier.wosWOS:001080496900001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.relation.ispartofJournal of Molecular Structureen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240519_kaen_US
dc.subjectNaproxen Ureaen_US
dc.subjectThiadiazole Ringen_US
dc.subjectTyrosinase Inhibitionen_US
dc.subjectCytotoxicityen_US
dc.subjectAnti-Migration Effecten_US
dc.subjectMolecular Dockingen_US
dc.titleSynthesis of naproxen thiadiazole urea hybrids and determination of their anti-melanoma, anti-migration, tyrosinase inhibitory activity, and molecular docking studiesen_US
dc.typeArticleen_US

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