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dc.contributor.authorSenkardes S.en_US
dc.contributor.authorKaushik-Basu N.en_US
dc.contributor.authorDurmaz I.en_US
dc.contributor.authorManvar D.en_US
dc.contributor.authorBasu A.en_US
dc.contributor.authorAtalay R.en_US
dc.contributor.authorGuniz Kucukguzel S.en_US
dc.date.accessioned2018-04-12T11:42:10Z
dc.date.available2018-04-12T11:42:10Z
dc.date.issued2016en_US
dc.identifier.issn2235234
dc.identifier.urihttp://hdl.handle.net/11693/37499
dc.description.abstractHepatitis C virus (HCV) infection is a main cause of chronic liver disease, leading to liver cirrhosis and hepatocellular carcinoma (HCC). The objective of our research was to develop effective agents against viral replication. We have previously identified the hydrazideehydrazone scaffold as a promising hepatitis C virus (HCV) and hepatocelluler inhibitor. Herein we describe the design a number of 20,40-difluoro-4-hydroxy-N'-(arylmethylidene) biphenyl-3-carbohydrazide (3a-t) as anti-HCV and anticancer agents. Results from evaluation of anti-HCV activity indicated that most of the synthesized hydrazone derivatives inhibited viral replication in the Huh7/Rep-Feo1b and Huh 7.5-FGR-JCI-Rluc2A reporter systems. Antiproliferative activities of increasing concentrations of 20,40-difluoro-4-hydroxy-N'-(2-pyridyl methylidene)biphenyl-3-carbohydrazide 3b and diflunisal (2.5e40 μM) were assessed in liver cancer cell lines (Huh7, HepG2, Hep3B, Mahlavu, FOCUS and SNU-475) with sulforhodamine B assay for 72 h. Compound 3b with 2-pyridinyl group in the hydrazone part exhibited promising cytotoxic activity against all cell lines with IC50 values of 10, 10.34 16.21 4.74, 9.29 and 8.33 μM for Huh7, HepG2, Hep3B, Mahlavu, FOCUS and SNU-475 cells, respectively, and produced dramatic cell cycle arrest at SubG1/G0 phase as an indicator of apoptotic cell death induction. © 2015 Elsevier Masson SAS.en_US
dc.language.isoEnglishen_US
dc.source.titleEuropean Journal of Medicinal Chemistryen_US
dc.relation.isversionofhttp://dx.doi.org/10.1016/j.ejmech.2015.10.041en_US
dc.subjectAntiviralen_US
dc.subjectDiflunisalen_US
dc.subjectHepatitis Cen_US
dc.subjectHepatocellular carcinomen_US
dc.subjectHydrazideehydrazoneen_US
dc.subject2',4' difluoro 4 hydroxy n' (arylmethylidene)biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(2 chloro 6 fluorophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(2 chlorophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(2,2 difluoro 1,3 benzodioxol 5 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(2,6 dichlorophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(2,6 difluorophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(3 bromophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(3 phenoxyphenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(3,4 dichlorophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(4 cyanophenyl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(5 ethylthiophen 2 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(5 methylthiophen 2 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(napthalen 1 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(napthalen 2 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(pyridin 2 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(pyridin 3 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(pyridin 4 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [(thiophen 2 yl)methylidene]biphenyl 3 carbohydrazideen_US
dc.subject2',4' difluoro 4 hydroxy n' [[4 (trifluoromethyl)phenyl]methylidene]biphenyl 3 carbohydrazideen_US
dc.subjectantineoplastic agenten_US
dc.subjectantivirus agenten_US
dc.subjectdiflunisalen_US
dc.subjecthydrazide derivativeen_US
dc.subjecthydrazone derivativeen_US
dc.subjectnonstructural protein 5Ben_US
dc.subjectunclassified drugen_US
dc.subject2',4'-difluoro-4-hydroxy-N'-(2-pyridylmethylidene)biphenyl-3-carbohydrazideen_US
dc.subjectantineoplastic agenten_US
dc.subjectantivirus agenten_US
dc.subjectdiflunisalen_US
dc.subjecthydrazine derivativeen_US
dc.subjecthydrazone derivativeen_US
dc.subjectantiproliferative activityen_US
dc.subjectantiviral activityen_US
dc.subjectapoptosisen_US
dc.subjectcell proliferationen_US
dc.subjectcell viabilityen_US
dc.subjectConference Paperen_US
dc.subjectcontrolled studyen_US
dc.subjectcytotoxicityen_US
dc.subjectDNA fragmentationen_US
dc.subjectdrug mechanismen_US
dc.subjectdrug synthesisen_US
dc.subjectG1 phase cell cycle checkpointen_US
dc.subjecthepatitis Cen_US
dc.subjectHepatitis C virusen_US
dc.subjectHepatitis C virus genotype 2en_US
dc.subjectHepG2 cell lineen_US
dc.subjecthumanen_US
dc.subjecthuman cellen_US
dc.subjectIC50en_US
dc.subjectliver cancer cell lineen_US
dc.subjectliver cell carcinomaen_US
dc.subjectnonhumanen_US
dc.subjectRNA replicationen_US
dc.subjectvirus replicationen_US
dc.subjectanalogs and derivativesen_US
dc.subjectCarcinoma, Hepatocellularen_US
dc.subjectchemical structureen_US
dc.subjectchemistryen_US
dc.subjectdose responseen_US
dc.subjectdrug effectsen_US
dc.subjectdrug screeningen_US
dc.subjectHepacivirusen_US
dc.subjectLiver Neoplasmsen_US
dc.subjectmicrobial sensitivity testen_US
dc.subjectpathologyen_US
dc.subjectstructure activity relationen_US
dc.subjectsynthesisen_US
dc.subjecttumor cell cultureen_US
dc.subjectAntineoplastic Agentsen_US
dc.subjectAntiviral Agentsen_US
dc.subjectApoptosisen_US
dc.subjectCarcinoma, Hepatocellularen_US
dc.subjectCell Proliferationen_US
dc.subjectDiflunisalen_US
dc.subjectDose-Response Relationship, Drugen_US
dc.subjectDrug Screening Assays, Antitumoren_US
dc.subjectHepacivirusen_US
dc.subjectHumansen_US
dc.subjectHydrazinesen_US
dc.subjectHydrazonesen_US
dc.subjectLiver Neoplasmsen_US
dc.subjectMicrobial Sensitivity Testsen_US
dc.subjectMolecular Structureen_US
dc.subjectStructure-Activity Relationshipen_US
dc.subjectTumor Cells, Cultureden_US
dc.titleSynthesis of novel diflunisal hydrazide-hydrazones as anti-hepatitis C virus agents and hepatocellular carcinoma inhibitorsen_US
dc.typeConference Paperen_US
dc.departmentDepartment of Molecular Biology and Genetics
dc.citation.spage301en_US
dc.citation.epage308en_US
dc.citation.volumeNumber108en_US
dc.identifier.doi10.1016/j.ejmech.2015.10.041en_US
dc.publisherElsevier Masson SASen_US


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