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

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dc.contributor.authorZENGİN KURT B.
dc.contributor.authorAltundağ Ö.
dc.contributor.authorTokgöz M. N.
dc.contributor.authorÖZTÜRK CİVELEK D.
dc.contributor.authorTuncay F. O.
dc.contributor.authorCakmak U.
dc.contributor.authorKOLCUOĞLU Y.
dc.contributor.authorAkdemir A.
dc.contributor.authorSönmez F.
dc.contributor.institutionauthorZENGİN KURT, BELMA
dc.contributor.institutionauthorÖZTÜRK CİVELEK, DİLEK
dc.date.accessioned2023-09-22T21:50:13Z
dc.date.available2023-09-22T21:50:13Z
dc.date.issued2023-01-01
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 μM 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 Ki value was calculated as 36.3 μM. 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 μM) showed the highest cytotoxicity on the HT-29 cells, while 3o (IC50 = 4.22 μM) exhibited the strongest cytotoxic effect on HepG2 cell lines. Also, 3j (IC50 = 7.55 μM 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.
dc.identifier.citationZENGİN KURT B., Altundağ Ö., Tokgöz M. N., ÖZTÜRK CİVELEK D., Tuncay F. O., Cakmak U., KOLCUOĞLU Y., Akdemir A., Sönmez F., "Synthesis of flurbiprofen thiadiazole urea derivatives and assessment of biological activities and molecular docking studies", Chemical Biology and Drug Design, 2023
dc.identifier.doi10.1111/cbdd.14336
dc.identifier.issn1747-0277
dc.identifier.pubmed37653693
dc.identifier.scopus85169317260
dc.identifier.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85169317260&origin=inward
dc.identifier.urihttps://hdl.handle.net/20.500.12645/38556
dc.relation.ispartofChemical Biology and Drug Design
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectEczacılık
dc.subjectTemel Eczacılık Bilimleri
dc.subjectYaşam Bilimleri
dc.subjectBiyoteknoloji
dc.subjectMoleküler Biyoloji ve Genetik
dc.subjectSitogenetik
dc.subjectKimya
dc.subjectBiyokimya
dc.subjectBiyoinorganik Kimya
dc.subjectSağlık Bilimleri
dc.subjectTemel Bilimler
dc.subjectPharmacology and Therapeutics
dc.subjectBasic Pharmaceutics Sciences
dc.subjectLife Sciences
dc.subjectBiotechnology
dc.subjectMolecular Biology and Genetics
dc.subjectCytogenetic
dc.subjectChemistry
dc.subjectBiochemistry
dc.subjectBioinorganic Chemistry
dc.subjectHealth Sciences
dc.subjectNatural Sciences
dc.subjectTemel Bilimler (SCI)
dc.subjectYaşam Bilimleri (LIFE)
dc.subjectFarmakoloji ve Toksikoloji
dc.subjectMikrobiyoloji
dc.subjectKİMYA, ORGANİK
dc.subjectFARMAKOLOJİ VE ECZACILIK
dc.subjectBİYOKİMYA VE MOLEKÜLER BİYOLOJİ
dc.subjectBİYOTEKNOLOJİ VE UYGULAMALI MİKROBİYOLOJİ
dc.subjectNatural Sciences (SCI)
dc.subjectLife Sciences (LIFE)
dc.subjectCHEMISTRY
dc.subjectPHARMACOLOGY & TOXICOLOGY
dc.subjectMOLECULAR BIOLOGY & GENETICS
dc.subjectMICROBIOLOGY
dc.subjectCHEMISTRY, ORGANIC
dc.subjectPHARMACOLOGY & PHARMACY
dc.subjectBIOCHEMISTRY & MOLECULAR BIOLOGY
dc.subjectBIOTECHNOLOGY & APPLIED MICROBIOLOGY
dc.subjectMoleküler Tıp
dc.subjectFarmakoloji
dc.subjectİlaç Keşfi
dc.subjectOrganik Kimya
dc.subjectFizik Bilimleri
dc.subjectMolecular Medicine
dc.subjectPharmacology
dc.subjectDrug Discovery
dc.subjectOrganic Chemistry
dc.subjectPhysical Sciences
dc.subjectcytotoxcity
dc.subjectflurbiprofen
dc.subjectmolecular docking
dc.subjectthiadiazole ring
dc.subjecttyrosinase inhibition
dc.subjecturea
dc.titleSynthesis of flurbiprofen thiadiazole urea derivatives and assessment of biological activities and molecular docking studies
dc.typearticle
dspace.entity.typePublication
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relation.isAuthorOfPublication821c461c-752b-4a78-a2e5-a6aaf5076b88
relation.isAuthorOfPublication.latestForDiscovery3fd265b5-fdd8-4c56-949b-deb0303c3db7

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