Article detail · 2015 · article
Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles
Data source split
- YÖKSİSYÖKSİS article record
- YÖKSİS venueJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Catalog match (ISSN)Journal of Enzyme Inhibition and Medicinal Chemistry
- OpenAlexOpenAlex enrichment (abstract, citations, topics)
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(50) value of 14.8 µM. 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(50) value of 4.29 µM. Therefore, compound 4a could be considered as a new anti-cancer and anti-HCV lead compound.
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Citations
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35citationsOpenAlex · cited_by_count (cache / database)
45 publications in the local catalog that cite this work (OpenAlex reference match; not the full global list).
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