ArticleActa pharmacologica Sinica2014
Discovering novel anti-HCV compounds with inhibitory activities toward HCV NS3/4A protease.
Article in Acta pharmacologica Sinica, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Development of a CRE/CREB-driven HBx responsive HBV cell culture reporter system for antiviral drug evaluation.JHEP reports : innovation in hepatology · 2025Article
- Development of a Noninfectious Japanese Encephalitis Virus Replicon for Antiviral Drug Screening and Gene Function Studies.Viruses · 2025Article
- Simultaneous Control of Endogenous and User-Defined Genetic Pathways Using Unique ecDHFR Pharmacological Chaperones.Cell chemical biology · 2020Article
- Betulin from Hedyotis hedyotidea ameliorates concanavalin A-induced and T cell-mediated autoimmune hepatitis in mice.Acta pharmacologica Sinica · 2017Article
- Identification and Analysis of Novel Inhibitors against NS3 Helicase and NS5B RNA-Dependent RNA Polymerase from Hepatitis C Virus 1b (Con1).Frontiers in microbiology · 2017Article
- Different Culture Metabolites of the Red Sea Fungus Fusarium equiseti Optimize the Inhibition of Hepatitis C Virus NS3/4A Protease (HCV PR).Marine drugs · 2016Article
- Discovery of Metal Ions Chelator Quercetin Derivatives with Potent Anti-HCV Activities.Molecules (Basel, Switzerland) · 2015Article
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo discover novel hepatitis C virus (HCV) inhibitors and elucidate the mechanism of action of the active compounds.
methodsHCV subgenomic replicon-based luciferase reporter cell line was used to screen 1200 synthetic compounds with novel structures. Huh7.5.1 cell line stably transfected with HCV NS3/4A protease reporter was established to investigate the anti-HCV mechanism of the active compounds. The active compounds were further examined in an in vitro HCV infection assay to confirm their anti-HCV activity.
resultsAfter two-round screening in the anti-HCV replicon assay, some 2,4-diaminoquinazoline derivatives and carboxamide analogues were found to possess anti-HCV replicon activities (the IC50 values were less than 5 μmol/L). Among them, two representative compounds HZ-1157 and LZ-110618-6 inhibited HCV NS3/4A protease with IC50 values of 1.0 and 0.68 μmol/L, respectively. Furthermore, HZ-1157 and LZ-110618-6 inhibited HCV infection in vitro with IC50 values of 0.82 and 0.11 μmol/L, respectively.
conclusionSome 2,4-diaminoquinazoline derivatives and carboxamide analogues have been identified as novel anti-HCV compounds.
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