Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles

Simple item page
dc.citation.epage785en_US
dc.citation.issueNumber5en_US
dc.citation.spage778en_US
dc.citation.volumeNumber30en_US
dc.contributor.authorÇikla-Süzgün P.en_US
dc.contributor.authorKaushik-Basu, N.en_US
dc.contributor.authorBasu, A.en_US
dc.contributor.authorArora P.en_US
dc.contributor.authorTalele, T.T.en_US
dc.contributor.authorDurmaz I.en_US
dc.contributor.authorÇetin-Atalay, R.en_US
dc.contributor.authorKüçükgüzel, S.G.en_US
dc.date.accessioned2016-02-08T09:40:34Z
dc.date.available2016-02-08T09:40:34Z
dc.date.issued2015en_US
dc.departmentDepartment of Molecular Biology and Geneticsen_US
dc.description.abstractArachidonic acid is an unsaturated fatty acid liberated from phospholipids of cell membranes. NSAIDs are known as targets of cyclooxygenase enzyme (COX-1, COX-2 and COX-3) in arachidonic acid metabolism. This mechanism of COX-2 in carcinogenesis causes cancer. In addition, COX-2 plays a role in the early stages of hepatocarcinogenesis. Hepatitis C virus (HCV) infection is cause of liver cirrhosis and hepatocellular carcinoma (HCC). The aim of our study was to improve effective agents against HCV. A novel series of new etodolac 1,2,4-triazoles derivatives (4a-h) have been synthesized and investigated for their activity against HCV NS5B polymerase. Compound 4a was found to be the most active with IC<inf>50</inf> value of 14.8 M. In accordance with these results, compound 4a was screened for anti-cancer activity on liver cancer cell lines (Huh7, Mahlavu, HepG2, FOCUS). Compound 4a showed anti-cancer activity against Huh7 human hepatoma cell line with IC<inf>50</inf> value of 4.29 M. Therefore, compound 4a could be considered as a new anti-cancer and anti-HCV lead compound. © 2015 Informa UK Ltd.en_US
dc.description.provenanceMade available in DSpace on 2016-02-08T09:40:34Z (GMT). No. of bitstreams: 1 bilkent-research-paper.pdf: 70227 bytes, checksum: 26e812c6f5156f83f0e77b261a471b5a (MD5) Previous issue date: 2015en
dc.identifier.doi10.3109/14756366.2014.971780en_US
dc.identifier.issn14756366
dc.identifier.urihttp://hdl.handle.net/11693/21070
dc.language.isoEnglishen_US
dc.publisherTaylor and Francis Ltden_US
dc.relation.isversionofhttp://dx.doi.org/10.3109/14756366.2014.971780en_US
dc.source.titleJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.subject1,2,4-Triazole-3-thioneen_US
dc.subjectetodolacen_US
dc.subjectHCV NS5B polymeraseen_US
dc.subjecthepatocellular carcinomaen_US
dc.subject5 [(1,8 diethyl 1,3,4,9 tetrahydropyrano[3,4 b]indole 1 yl) methyl] 4 benzyl 2,4 dihydro 3h 1,2,4 triazole 3 thioneen_US
dc.subject5 [(1,8 diethyl 1,3,4,9 tetrahydropyrano[3,4 b]indole 1 yl) methyl] 4 methyl 2,4 dihydro 3h 1,2,4 triazole 3 thioneen_US
dc.subjectantivirus agenten_US
dc.subjectcyclooxygenase 1en_US
dc.subjectcyclooxygenase 2en_US
dc.subjectetodolacen_US
dc.subjectnonstructural protein 5Ben_US
dc.subjecttriazole derivativeen_US
dc.subjectunclassified drugen_US
dc.subjectantineoplastic activityen_US
dc.subjectantiviral activityen_US
dc.subjectArticleen_US
dc.subjectdrug synthesisen_US
dc.subjectgrowth inhibitionen_US
dc.subjectHepatitis C virusen_US
dc.subjecthepatocellular carcinoma cell lineen_US
dc.subjecthumanen_US
dc.subjecthuman cellen_US
dc.subjectIC50en_US
dc.subjectliver cancer cell lineen_US
dc.subjectpriority journalen_US
dc.subjectvirus infectionen_US
dc.titleAnti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazolesen_US
dc.typeArticleen_US

Files

Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles.pdf
Size:
826.52 KB
Format:
Adobe Portable Document Format
Description:
Full printable version
Download

Collections

Department of Molecular Biology and Genetics