Synthesis and antiproliferative evaluation of new 1,3,5-trisubstituted 1,2,4-triazole derivatives against glioblastoma cell lines

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dc.authorid0000-0001-6975-6808
dc.authorid0000-0003-0957-6965
dc.contributor.authorKoç, Elif Beyza
dc.contributor.authorSucu, Bilgesu Onur
dc.date.accessioned2023-05-26T07:15:49Z
dc.date.available2023-05-26T07:15:49Z
dc.date.issued2023
dc.departmentİstanbul Medipol Üniversitesi, Rektörlük, Sağlık Bilim ve Teknolojileri Araştırma Enstitüsü
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.description.abstractA series of novel 1,3,5-trisubstituted-1,2,4-triazole derivatives were successfully synthesized from the starting materials of caffeic acid (CA) and ferulic acid (FA) in moderate to good yields (45-71 %). All novel compounds were screened for antiproliferative activity against three glioblastoma (GB) cell lines. Several compounds exhibited improved cytotoxic activities compared to the caffeic acid phenethyl ester (CAPE). Among the novel derivatives, 4-(2-(1-benzyl-3-phenyl-1H-1,2,4-triazol-5-yl)vinyl)-2-methoxyphenol (4) exhibited the most potent activity against the U87G, T98G and LN229 cell lines. Western blot results showed significantly reduced poly(ADP-ribose) polymerase (PARP) and increased the Bcl-2-associated X (Bax) protein levels in T98G cells. Also, flow cytometry results using Annexin-V/Propidium Iodide (PI) staining indicated that apoptosis was induced in T98G cells. It was found to be a promising drug candidate with strong physicochemical and bioavailability properties as a result of SwissADME calculations. These results show that novel compounds containing a 1,2,4-triazole moiety have a good antiproliferative activity on GB cells.
dc.identifier.citationKoç, E. B. ve Sucu, B. O. (2023). Synthesis and antiproliferative evaluation of new 1,3,5-trisubstituted 1,2,4-triazole derivatives against glioblastoma cell lines. ChemistrySelect, 8(18). https://doi.org/10.1002/slct.202300411
dc.identifier.doi10.1002/slct.202300411
dc.identifier.issn2365-6549
dc.identifier.issue18
dc.identifier.scopus2-s2.0-85159115459
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1002/slct.202300411
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10975
dc.identifier.volume8
dc.identifier.wos000984445500001en_US
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.institutionauthorKoç, Elif Beyza
dc.institutionauthorSucu, Bilgesu Onur
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofChemistrySelecten_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.relation.tubitakinfo:eu-repo/grantAgreement/TUBITAK/SOBAG/119Z116
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectAntiproliferativeactivity
dc.subjectCaffeicacidphenethylester(CAPE)
dc.subjectGlioblastomamultiform(GB)
dc.subjectOnepotsynthesis
dc.subject1,2,4-Triazole
dc.titleSynthesis and antiproliferative evaluation of new 1,3,5-trisubstituted 1,2,4-triazole derivatives against glioblastoma cell lines
dc.typeArticle

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