ArticleJournal of medicinal chemistry2011
Discovery of naturally occurring aurones that are potent allosteric inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 117 citations in OpenAlex.
- Hispidol Regulates Behavioral Responses to Ethanol through Modulation of BK Channels: A Novel Candidate for the Treatment of Alcohol Use Disorder.Molecules (Basel, Switzerland) · 2024Article
- Research status of indole-modified natural products.RSC medicinal chemistry · 2023Review
- Design, synthesis and anticancer evaluation of polymethoxy aurones as potential cell cycle inhibitors.Heliyon · 2023Article
- Evaluation of the Antibacterial Effect of Aurone-Derived Triazoles onAntibiotics (Basel, Switzerland) · 2023Article
- Anti-viral triterpenes: a review.Phytochemistry reviews : proceedings of the Phytochemical Society of Europe · 2022Review
- Recent advances in the discovery of potent RNA-dependent RNA-polymerase (RdRp) inhibitors targeting viruses.RSC medicinal chemistry · 2021Review
- Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations.Molecules (Basel, Switzerland) · 2020Article
- Semisynthetic aurones inhibit tubulin polymerization at the colchicine-binding site and repress PC-3 tumor xenografts in nude mice and myc-induced T-ALL in zebrafish.Scientific reports · 2019Article
- High-content imaging assay to evaluate Toxoplasma gondii infection and proliferation: A multiparametric assay to screen new compounds.PloS one · 2018Article
- 2-Hydroxypyridine-ACS medicinal chemistry letters · 2017Article
- Combinatorial Synthesis of Structurally Diverse Triazole-Bridged Flavonoid Dimers and Trimers.Molecules (Basel, Switzerland) · 2016Article
- Chemical constituents from the rhizomes of Smilax glabra and their antimicrobial activity.Molecules (Basel, Switzerland) · 2013Article
- Aurones: a promising heterocyclic scaffold for the development of potent antileishmanial agents.International journal of medicinal chemistry · 2012Article
- Amino acid-derived defense metabolites from plants: A potential source to facilitate novel antimicrobial development.The Journal of biological chemistryReview
Corrections and comments
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Authors and funding
10 authors at 6 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have identified naturally occurring 2-benzylidenebenzofuran-3-ones (aurones) as new templates for non-nucleoside hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors. The aurone target site, identified by site-directed mutagenesis, is located in thumb pocket I of HCV RdRp. The RdRp inhibitory activity of 42 aurones was rationally explored in an enzyme assay. Molecular docking studies were used to determine how aurones bind to HCV RdRp and to predict their range of inhibitory activity. Seven aurone derivatives were found to have potent inhibitory effects on HCV RdRp, with IC(50) below 5 μM and excellent selectivity index (inhibition activity versus cellular cytotoxicity). The most active aurone analogue was (Z)-2-((1-butyl-1H-indol-3-yl)methylene)-4,6-dihydroxybenzofuran-3(2H)-one (compound 51), with an IC(50) of 2.2 μM. Their potent RdRp inhibitory activity and their low toxicity make these molecules attractive candidates as direct-acting anti-HCV agents.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.