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

Simple item page
dc.contributor.authorSÜZGÜN, PELİN
dc.contributor.authorsCikla-Suzgun, Pelin; Kaushik-Basu, Neerja; Basu, Amartya; Arora, Payal; Talele, Tanaji T.; Durmaz, Irem; Cetin-Atalay, Rengul; Kucukguzel, S. Guniz
dc.date.accessioned2022-03-14T11:07:25Z
dc.date.available2022-03-14T11:07:25Z
dc.date.issued2015-09-03
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 IC50 value of 14.8 mu 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 IC50 value of 4.29 mu M. Therefore, compound 4a could be considered as a new anti-cancer and anti-HCV lead compound.
dc.identifier.doi10.3109/14756366.2014.971780
dc.identifier.eissn1475-6374
dc.identifier.issn1475-6366
dc.identifier.pubmed25676325
dc.identifier.urihttps://hdl.handle.net/11424/245919
dc.identifier.wosWOS:000361328700009
dc.language.isoeng
dc.publisherTAYLOR & FRANCIS LTD
dc.relation.ispartofJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subject1,2,4-Triazole-3-thione
dc.subjectetodolac
dc.subjectHCV NS5B polymerase
dc.subjecthepatocellular carcinoma
dc.subjectHUMAN HEPATOCELLULAR-CARCINOMA
dc.subjectDERIVATIVES
dc.subjectCYCLOOXYGENASE-2
dc.subjectCYTOTOXICITY
dc.subjectINHIBITION
dc.subjectDISCOVERY
dc.subjectHYDRAZIDE
dc.titleAnti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles
dc.typearticle
dspace.entity.typePublication
local.avesis.idecdf3370-b43d-4a25-8967-980bca616188
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.indexed.atPUBMED
local.journal.numberofpages8
oaire.citation.endPage785
oaire.citation.issue5
oaire.citation.startPage778
oaire.citation.titleJOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
oaire.citation.volume30
relation.isAuthorOfPublication6f8a150f-0ec8-4a51-9a1b-b9c26aecdf69
relation.isAuthorOfPublication.latestForDiscovery6f8a150f-0ec8-4a51-9a1b-b9c26aecdf69

Files

Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
Çıkla-Süzgün et al. - 2015 - Anti-cancer and anti-hepatitis C virus NS5B polyme.pdf
Size:
826.52 KB
Format:
Adobe Portable Document Format
Download

Collections

Research Outputs