ArticleEuropean journal of medicinal chemistry2012
Inhibition of hepatitis C virus NS5B polymerase by S-trityl-L-cysteine derivatives.
Article in European journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 20 citations in OpenAlex.
- Dithiophosphate-Induced Redox Conversions of Reduced and Oxidized Glutathione.Molecules (Basel, Switzerland) · 2021Article
- Triphenylphosphonium Moiety Modulates Proteolytic Stability and Potentiates Neuroprotective Activity of Antioxidant TetrapeptidesFrontiers in pharmacology · 2018Article
- New pyrazolobenzothiazine derivatives as hepatitis C virus NS5B polymerase palm site I inhibitors.Journal of medicinal chemistry · 2014Article
- The versatile nature of the 6-aminoquinolone scaffold: identification of submicromolar hepatitis C virus NS5B inhibitors.Journal of medicinal chemistry · 2014Article
- 2-Heteroarylimino-5-arylidene-4-thiazolidinones as a new class of non-nucleoside inhibitors of HCV NS5B polymerase.European journal of medicinal chemistry · 2013Article
- Structure-based discovery of pyrazolobenzothiazine derivatives as inhibitors of hepatitis C virus replication.Journal of medicinal chemistry · 2013Article
- Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.Journal of medicinal chemistry · 2013Article
- Discovery of new scaffolds for rational design of HCV NS5B polymerase inhibitors.European journal of medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
11 authors at 7 institutions in 6 countries.
Funding
Abstract
Structure-based studies led to the identification of a constrained derivative of S-trityl-l-cysteine (STLC) scaffold as a candidate inhibitor of hepatitis C virus (HCV) NS5B polymerase. A panel of STLC derivatives were synthesized and investigated for their activity against HCV NS5B. Three STLC derivatives, 9, F-3070, and F-3065, were identified as modest HCV NS5B inhibitors with IC(50) values between 22.3 and 39.7 μM. F-3070 and F-3065 displayed potent inhibition of intracellular NS5B activity in the BHK-NS5B-FRLuc reporter and also inhibited HCV RNA replication in the Huh7/Rep-Feo1b reporter system. Binding mode investigations suggested that the STLC scaffold can be used to develop new NS5B inhibitors by further chemical modification at one of the trityl phenyl group.
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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.