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

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      Author
      Çikla-Süzgün P.
      Kaushik-Basu, N.
      Basu, A.
      Arora P.
      Talele, T.T.
      Durmaz I.
      Çetin-Atalay, R.
      Küçükgüzel, S.G.
      Date
      2015
      Source Title
      Journal of Enzyme Inhibition and Medicinal Chemistry
      Print ISSN
      14756366
      Publisher
      Taylor and Francis Ltd
      Volume
      30
      Issue
      5
      Pages
      778 - 785
      Language
      English
      Type
      Article
      Item Usage Stats
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      144
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      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.
      Keywords
      1,2,4-Triazole-3-thione
      etodolac
      HCV NS5B polymerase
      hepatocellular carcinoma
      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
      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
      antivirus agent
      cyclooxygenase 1
      cyclooxygenase 2
      etodolac
      nonstructural protein 5B
      triazole derivative
      unclassified drug
      antineoplastic activity
      antiviral activity
      Article
      drug synthesis
      growth inhibition
      Hepatitis C virus
      hepatocellular carcinoma cell line
      human
      human cell
      IC50
      liver cancer cell line
      priority journal
      virus infection
      Permalink
      http://hdl.handle.net/11693/21070
      Published Version (Please cite this version)
      http://dx.doi.org/10.3109/14756366.2014.971780
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