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dc.contributor.authorEfeoğlu, Çağla
dc.contributor.authorYetkin, Derya
dc.contributor.authorNural, Yahya
dc.contributor.authorEce, Abdulilah
dc.contributor.authorSeferoğlu, Zeynel
dc.contributor.authorAyaz, Furkan
dc.date.accessioned2022-05-31T08:03:02Z
dc.date.available2022-05-31T08:03:02Z
dc.date.issued15.09.2022en_US
dc.identifier.issn00222860
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2022.133284
dc.identifier.urihttps://hdl.handle.net/20.500.12445/2143
dc.description.abstractIn this study, four novel urea-thiourea hybrids bearing 1,4-naphthoquinone moiety were synthesized by the reaction of 2,3-diaminonaphthalene-1,4-dione and various isothiocyanate derivatives in 75–88% yield, and their molecular structures were characterized by using 1H/13C NMR, FT-IR and HRMS techniques. Urea-thiourea hybrids have been known for their anti-inflammatory activities. Therefore, in our study, we aimed to decipher their biological activities on mammalian macrophages. Macrophages were stimulated by LPS and pro-inflammatory TNF, IL6, GMCSF and IL12p40 cytokine production levels were measured in the presence of these derivatives by ELISA. Our results suggest that these derivatives on stimulated mammalian macrophages had anti-inflammatory activities. In order to examine their intracellular mechanism of action, intracellular phosphorylated (activated) PI3K protein levels were measured in the presence of our novel derivatives by flow cytometry. Our results suggest that these novel derivatives had anti-inflammatory activities on mammalian macrophages by blocking the PI3K activation and decreasing the production of pro-inflammatory cytokines. Molecular docking calculations were also employed to elucidate the theoretical binding modes of our studied compounds with PI3Kγ . These derivatives have the potential to be utilized as anti-inflammatory drug agents against versatile inflammatory and autoimmune disorders.en_US
dc.language.isoengen_US
dc.publisherElsevieren_US
dc.relation.isversionofhttps://doi.org/10.1016/j.molstruc.2022.133284en_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectAnti-Inflammatory Activityen_US
dc.subjectThioureaen_US
dc.subject1,4-Naphthoquinoneen_US
dc.subjectMacrophagesen_US
dc.subjectInflammationen_US
dc.subjectPI3K Pathwayen_US
dc.titleNovel urea-thiourea hybrids bearing 1,4-naphthoquinone moiety: Anti-inflammatory activity on mammalian macrophages by regulating intracellular PI3K pathway, and molecular docking studyen_US
dc.typearticleen_US
dc.relation.journalJournal of Molecular Structureen_US
dc.contributor.departmentEczacılık Fakültesien_US
dc.identifier.volume1264en_US
dc.identifier.startpage1en_US
dc.identifier.endpage9en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


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