Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles
dc.citation.epage | 785 | en_US |
dc.citation.issueNumber | 5 | en_US |
dc.citation.spage | 778 | en_US |
dc.citation.volumeNumber | 30 | en_US |
dc.contributor.author | Çikla-Süzgün P. | en_US |
dc.contributor.author | Kaushik-Basu, N. | en_US |
dc.contributor.author | Basu, A. | en_US |
dc.contributor.author | Arora P. | en_US |
dc.contributor.author | Talele, T.T. | en_US |
dc.contributor.author | Durmaz I. | en_US |
dc.contributor.author | Çetin-Atalay, R. | en_US |
dc.contributor.author | Küçükgüzel, S.G. | en_US |
dc.date.accessioned | 2016-02-08T09:40:34Z | |
dc.date.available | 2016-02-08T09:40:34Z | |
dc.date.issued | 2015 | en_US |
dc.department | Department of Molecular Biology and Genetics | en_US |
dc.description.abstract | Arachidonic 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.provenance | Made 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: 2015 | en |
dc.identifier.doi | 10.3109/14756366.2014.971780 | en_US |
dc.identifier.issn | 14756366 | |
dc.identifier.uri | http://hdl.handle.net/11693/21070 | |
dc.language.iso | English | en_US |
dc.publisher | Taylor and Francis Ltd | en_US |
dc.relation.isversionof | http://dx.doi.org/10.3109/14756366.2014.971780 | en_US |
dc.source.title | Journal of Enzyme Inhibition and Medicinal Chemistry | en_US |
dc.subject | 1,2,4-Triazole-3-thione | en_US |
dc.subject | etodolac | en_US |
dc.subject | HCV NS5B polymerase | en_US |
dc.subject | hepatocellular carcinoma | en_US |
dc.subject | 5 [(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 thione | en_US |
dc.subject | 5 [(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 thione | en_US |
dc.subject | antivirus agent | en_US |
dc.subject | cyclooxygenase 1 | en_US |
dc.subject | cyclooxygenase 2 | en_US |
dc.subject | etodolac | en_US |
dc.subject | nonstructural protein 5B | en_US |
dc.subject | triazole derivative | en_US |
dc.subject | unclassified drug | en_US |
dc.subject | antineoplastic activity | en_US |
dc.subject | antiviral activity | en_US |
dc.subject | Article | en_US |
dc.subject | drug synthesis | en_US |
dc.subject | growth inhibition | en_US |
dc.subject | Hepatitis C virus | en_US |
dc.subject | hepatocellular carcinoma cell line | en_US |
dc.subject | human | en_US |
dc.subject | human cell | en_US |
dc.subject | IC50 | en_US |
dc.subject | liver cancer cell line | en_US |
dc.subject | priority journal | en_US |
dc.subject | virus infection | en_US |
dc.title | Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles | en_US |
dc.type | Article | en_US |
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