Synthesis of flurbiprofen thiadiazole urea derivatives and assessment of biological activities and molecular docking studies

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dc.authoridOzturk Civelek, Dilek/0000-0003-2485-891X
dc.authoridSönmez, Fatih/0000-0001-7486-6374
dc.authoridçakmak, Ümmühan/0000-0001-8719-2436
dc.authoridKurt, Belma Zengin/0000-0002-4663-5402
dc.authoridAkdemir, Atilla/0000-0001-8416-0471
dc.authoridTokgoz, Merve Nur/0009-0004-5332-0857
dc.authorwosidOzturk Civelek, Dilek/AAD-9249-2020
dc.authorwosidSönmez, Fatih/AAR-5428-2020
dc.authorwosidçakmak, Ümmühan/AAJ-7614-2021
dc.authorwosidKurt, Belma Zengin/W-9070-2019
dc.authorwosidAkdemir, Atilla/G-2595-2015
dc.contributor.authorKurt, Belma Zengin
dc.contributor.authorAltundag, Ozlem
dc.contributor.authorTokgoz, Merve Nur
dc.contributor.authorCivelek, Dilek Ozturk
dc.contributor.authorTuncay, Fulya Oz
dc.contributor.authorCakmak, Ummuhan
dc.contributor.authorKolcuoglu, Yakup
dc.date.accessioned2024-05-19T14:40:38Z
dc.date.available2024-05-19T14:40:38Z
dc.date.issued2023
dc.departmentİstinye Üniversitesien_US
dc.description.abstractTotally 15 novel flurbiprofen urea derivatives were synthesized bearing the thiadiazole ring. Their inhibition effects on tyrosinase were determined. 3c was found to be the strongest inhibitor with the IC50 value of 68.0 mu M against tyrosinase. The enzyme inhibition types of the synthesized compounds were determined by examining the kinetic parameters. The inhibition type of 3c was determined as uncompetitive and the K-i value was calculated as 36.3 mu M. Moreover, their cytotoxic effects on hepatocellular carcinoma (HepG2), colorectal carcinoma (HT-29), and melanoma (B16F10) cell lines were evaluated. According to the cytotoxicity results, 3l (IC50 = 14.11 mu M) showed the highest cytotoxicity on the HT-29 cells, while 3o (IC50 = 4.22 mu M) exhibited the strongest cytotoxic effect on HepG2 cell lines. Also, 3j (IC50 = 7.55 mu M strongly affected B16F10. The effects of synthesized compounds on the healthy cell line were evaluated on the CCD-986Sk cell line. Molecular modelling studies have indicated the potential binding interactions of the uncompetitive inhibitor 3c with the enzyme-substrate complex.en_US
dc.description.sponsorshipBezmialem Vakif Universitesien_US
dc.description.sponsorshipBezmialem Vakif Universitesien_US
dc.identifier.doi10.1111/cbdd.14336
dc.identifier.endpage1468en_US
dc.identifier.issn1747-0277
dc.identifier.issn1747-0285
dc.identifier.issue6en_US
dc.identifier.pmid37653693en_US
dc.identifier.scopus2-s2.0-85169317260en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.startpage1458en_US
dc.identifier.urihttps://doi.org10.1111/cbdd.14336
dc.identifier.urihttps://hdl.handle.net/20.500.12713/4991
dc.identifier.volume102en_US
dc.identifier.wosWOS:001065019700001en_US
dc.identifier.wosqualityN/Aen_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.relation.ispartofChemical Biology & Drug Designen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.snmz20240519_kaen_US
dc.subjectCytotoxcityen_US
dc.subjectFlurbiprofenen_US
dc.subjectMolecular Dockingen_US
dc.subjectThiadiazole Ringen_US
dc.subjectTyrosinase Inhibitionen_US
dc.subjectUreaen_US
dc.titleSynthesis of flurbiprofen thiadiazole urea derivatives and assessment of biological activities and molecular docking studiesen_US
dc.typeArticleen_US

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