In vitro cytotoxic and in vivo antitumoral activities of some aminomethyl derivatives of 2,4-dihydro-3H-1,2,4-triazole-3-thiones-Evaluation of their acetylcholinesterase and carbonic anhydrase enzymes inhibition profiles

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dc.authoridGulcin, ilhami/0000-0001-5993-1668
dc.authoridKoparir, Metin/0000-0003-1031-783X
dc.authoridÇERİBAŞI, Ali Osman/0000-0002-6096-4042
dc.authoridKaratepe, Mustafa/0000-0001-6358-5913
dc.authoridSandal, Suleyman/0000-0002-8916-3329
dc.authoridÇERİBAŞI, Ali Osman/0000-0002-6096-4042
dc.authoridTaslimi, Parham/0000-0002-3171-0633
dc.authorwosidGulcin, ilhami/F-1428-2014
dc.authorwosidKoparir, Metin/W-7674-2018
dc.authorwosidÇERİBAŞI, Ali Osman/JCE-2165-2023
dc.authorwosidKaratepe, Mustafa/HII-5655-2022
dc.authorwosidDaştan, Taner/AAB-3640-2021
dc.authorwosidSandal, Suleyman/AAA-6388-2021
dc.authorwosidTaslimi, Parham/AAL-2788-2020
dc.contributor.authorTimur, Irfan
dc.contributor.authorKocyigit, Umit M.
dc.contributor.authorDastan, Taner
dc.contributor.authorSandal, Suleyman
dc.contributor.authorCeribasi, Ali Osman
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2024-08-04T20:45:31Z
dc.date.available2024-08-04T20:45:31Z
dc.date.issued2019
dc.departmentİnönü Üniversitesien_US
dc.description.abstractThe 1,2,4-triazole and its derivatives were reported to exhibit various pharmacological activities such as antimicrobial, analgesic, anti-inflammatory, antitumoural, cytotoxic, and antioxidant properties. In this study, a series of triazole compounds (M1-M10) were evaluated for some biological activities. In vitro qualifications of these compounds on acetylcholinesterase (AChE) and human carbonic anhydrase enzyme activities were performed. Also, their antitumoral activities in human colon cancer (HT29) cell line cultures were examined. In addition, colon cancer experimentation was induced in rats by an in vivo method, and the in vivo anticancer effects of triazole derivatives were investigated. Also, the effects of these derivatives in levels of antioxidant vitamin A, vitamin E, and MDA were studied in rat liver and blood samples. Most of the compounds were found to exhibit significant antioxidant and antitumoral activities. All the compounds had cytotoxic activities on HT29 cell lines with their IC50 values lower than 10 mu M concentrations. The low IC50 values of the compounds are M1 (3.88 mu M), M2 (2.18 mu M), M3 (4.2 mu M), M4 (2.58 mu M), M5 (2.88 mu M), M6 (2.37 mu M), M7 (3.49 mu M), M8 (4.01 mu M), M9 (8.90 mu M), and M10 (3.12 mu M).en_US
dc.identifier.doi10.1002/jbt.22239
dc.identifier.issn1095-6670
dc.identifier.issn1099-0461
dc.identifier.issue1en_US
dc.identifier.pmid30368973en_US
dc.identifier.scopus2-s2.0-85055710438en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/jbt.22239
dc.identifier.urihttps://hdl.handle.net/11616/98514
dc.identifier.volume33en_US
dc.identifier.wosWOS:000455510900008en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWileyen_US
dc.relation.ispartofJournal of Biochemical and Molecular Toxicologyen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectantitumoural activityen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectenzyme inhibitionen_US
dc.subjectMDAen_US
dc.subjecttriazoleen_US
dc.titleIn vitro cytotoxic and in vivo antitumoral activities of some aminomethyl derivatives of 2,4-dihydro-3H-1,2,4-triazole-3-thiones-Evaluation of their acetylcholinesterase and carbonic anhydrase enzymes inhibition profilesen_US
dc.typeArticleen_US

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