Synthesis and Characterization of Celecoxib Derivatives as Possible Anti-Inflammatory, Analgesic, Antioxidant, Anticancer and Anti-HCV Agents

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dc.authoridsenkardes, sevil/0000-0002-0523-459X
dc.authoridKüçükgüzel, Ş.Güniz/0000-0001-9405-8905
dc.authoridUniversity, Aydin Adnan Menderes/0000-0002-9325-3757
dc.authoridOzakpınar, Ozlem Bingol/0000-0003-0287-5639
dc.authoridAKTAY, Goknur/0000-0002-1646-8674
dc.authorwosidGürsoy, Şule/JPW-8593-2023
dc.authorwosidsenkardes, sevil/AAA-3948-2020
dc.authorwosidKüçükgüzel, Ş.Güniz/AAQ-8954-2021
dc.authorwosidUniversity, Aydin Adnan Menderes/Z-2790-2019
dc.authorwosidOzakpınar, Ozlem Bingol/ABI-4144-2020
dc.authorwosidOzakpinar, Ozlem Bingol/ACB-1160-2022
dc.contributor.authorKucukguzel, S. Guniz
dc.contributor.authorCoskun, Inci
dc.contributor.authorAydin, Sevil
dc.contributor.authorAktay, Goknur
dc.contributor.authorGursoy, Sule
dc.contributor.authorCevik, Ozge
dc.contributor.authorOzakpinar, Ozlem Bingol
dc.date.accessioned2024-08-04T20:37:29Z
dc.date.available2024-08-04T20:37:29Z
dc.date.issued2013
dc.departmentİnönü Üniversitesien_US
dc.description.abstractA series of novel N-(3-substituted aryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides 2a-e were synthesized by the addition of ethyl alpha-bromoacetate and anhydrous sodium acetate in dry ethanol to N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)-3-(trifluoro-methyl)- 1H-pyrazol-1-yl] benzene sulfonamides 1a-e, which were synthesized by the reaction of alkyl/aryl isothiocyanates with celecoxib. The structures of the isolated products were determined by spectral methods and their anti-inflammatory, analgesic, antioxidant, anticancer and anti-HCV NS5B RNA-dependent RNA polymerase (RdRp) activities evaluated. The compounds were also tested for gastric toxicity and selected compound 1a was screened for its anticancer activity against 60 human tumor cell lines. These investigations revealed that compound 1a exhibited anti-inflammatory and analgesic activities and further did not cause tissue damage in liver, kidney, colon and brain compared to untreated controls or celecoxib. Compounds 1c and 1d displayed modest inhibition of HCV NS5B RdRp activity. In conclusion, N-(ethylcarbamothioyl)-4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide (1a) may have the potential to be developed into a therapeutic agent.en_US
dc.description.sponsorshipResearch Fund of Marmara University [SAG-A-310510-0175]; National Institute of Health [CA153147]en_US
dc.description.sponsorshipWe wish to thank the National Cancer Institute for in vitro pharmacological screening. This work was generously supported by the Research Fund of Marmara University, project number: SAG-A-310510-0175 to S. G. K. HCV NS5B inhibition studies were supported by the National Institute of Health Research Grant CA153147 to N.K.-B. The authors are grateful to Jurgen Gross from the Institute of Organic Chemistry, University of Heidelberg, for his generous help on obtaining HR-EI mass spectra of the synthesized compounds.en_US
dc.identifier.doi10.3390/molecules18033595
dc.identifier.endpage3614en_US
dc.identifier.issn1420-3049
dc.identifier.issue3en_US
dc.identifier.pmid23519201en_US
dc.identifier.scopus2-s2.0-84875601300en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage3595en_US
dc.identifier.urihttps://doi.org/10.3390/molecules18033595
dc.identifier.urihttps://hdl.handle.net/11616/95994
dc.identifier.volume18en_US
dc.identifier.wosWOS:000316611700079en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherMdpien_US
dc.relation.ispartofMoleculesen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectanti-inflammatoryen_US
dc.subjectanticanceren_US
dc.subjectcelecoxiben_US
dc.subjecthepatitis C NS5Ben_US
dc.subjectsulfonylthioureaen_US
dc.titleSynthesis and Characterization of Celecoxib Derivatives as Possible Anti-Inflammatory, Analgesic, Antioxidant, Anticancer and Anti-HCV Agentsen_US
dc.typeArticleen_US

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