Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1, 2, 4-triazoles*. (October 2015)

• Record Type: Journal Article
• Authors: Çıkla-Süzgün, Pelin; Kaushik-Basu, Neerja; Basu, Amartya; Arora, Payal; Talele, Tanaji T.; Durmaz, Irem; Çetin-Atalay, Rengül; Küçükgüzel, Ş.Güniz
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 30:Number 5(2015:Oct.)
• Page Start: 778
• Page End: 785
• Publication Date: 2015-10
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title>Abstract</title> <p>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 (<bold>4a</bold>–<bold>h</bold>) have been synthesized and investigated for their activity against HCV NS5B polymerase. Compound <bold>4a</bold> was found to be the most active with IC₅₀ value of 14.8 µM. In accordance with these results, compound <bold>4a</bold> was screened for anti-cancer activity on liver cancer cell lines (Huh7, Mahlavu, HepG2, FOCUS). Compound <bold>4a</bold> showed anti-cancer activity against Huh7 human hepatoma cell line with IC₅₀ value of 4.29 µM. Therefore, compound <bold>4a</bold> could be considered as a new anti-cancer and anti-HCV lead compound.</p> </abstract>