Synthesis of novel diflunisal hydrazide-hydrazones as anti-hepatitis C virus agents and hepatocellular carcinoma inhibitors

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dc.citation.epage308en_US
dc.citation.spage301en_US
dc.citation.volumeNumber108en_US
dc.contributor.authorŞenkardeş, S.en_US
dc.contributor.authorKaushik-Basu, N.en_US
dc.contributor.authorDurmaz, İremen_US
dc.contributor.authorManvar, D.en_US
dc.contributor.authorBasu, A.en_US
dc.contributor.authorAtalay, R.en_US
dc.contributor.authorKüçükgüzel, Ş. Günizen_US
dc.coverage.spatialİstanbul, Turkeyen_US
dc.date.accessioned2018-04-12T11:42:10Zen_US
dc.date.available2018-04-12T11:42:10Zen_US
dc.date.issued2016en_US
dc.departmentDepartment of Molecular Biology and Geneticsen_US
dc.descriptionDate of Conference: 18-23 September 2014en_US
dc.descriptionConference Name: 4th International Meeting on Pharmacy and Pharmaceutical and Sciences, 2014en_US
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.en_US
dc.identifier.doi10.1016/j.ejmech.2015.10.041en_US
dc.identifier.issn0223-5234en_US
dc.identifier.urihttp://hdl.handle.net/11693/37499en_US
dc.language.isoEnglishen_US
dc.publisherElsevieren_US
dc.relation.isversionofhttp://dx.doi.org/10.1016/j.ejmech.2015.10.041en_US
dc.source.titleEuropean Journal of Medicinal Chemistryen_US
dc.subjectAntiviralen_US
dc.subjectDiflunisalen_US
dc.subjectHepatitis Cen_US
dc.subjectHepatocellular carcinomen_US
dc.subjectHydrazide-hydrazoneen_US
dc.titleSynthesis of novel diflunisal hydrazide-hydrazones as anti-hepatitis C virus agents and hepatocellular carcinoma inhibitorsen_US
dc.typeConference Paperen_US
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