ArticleJournal of medicinal chemistry2011
Discovery, synthesis, and biological evaluation of a novel group of selective inhibitors of filoviral entry.
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 26 papers.
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Who cites it
26 citing papers in PubMed, 73 citations in OpenAlex.
- Pseudotyped Viruses for Marburgvirus and Ebolavirus.Advances in experimental medicine and biology · 2023Article
- Therapeutic Strategies against Ebola Virus Infection.Viruses · 2022Review
- Ebola Virus Entry Inhibitors.Advances in experimental medicine and biology · 2022Article
- Pyrrolo[2',3':3,4]cyclohepta[1,2-Journal of medicinal chemistry · 2020Article
- Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.Journal of medicinal chemistry · 2020Article
- Toward the Target: Tilorone, Quinacrine, and Pyronaridine Bind to Ebola Virus Glycoprotein.ACS medicinal chemistry letters · 2020Article
- Structure-Based in Silico Screening Identifies a Potent Ebolavirus Inhibitor from a Traditional Chinese Medicine Library.Journal of medicinal chemistry · 2019Article
- Article
- Computer-Aided Discovery and Characterization of Novel Ebola Virus Inhibitors.Journal of medicinal chemistry · 2018Article
- Target Identification and Mode of Action of Four Chemically Divergent Drugs against Ebolavirus Infection.Journal of medicinal chemistry · 2018Article
- N-Heterocyclic borneol derivatives as inhibitors of Marburg virus glycoprotein-mediated VSIV pseudotype entry.MedChemComm · 2017Article
- A bioluminescent imaging mouse model for Marburg virus based on a pseudovirus system.Human vaccines & immunotherapeutics · 2017Article
- Selective inhibition of Ebola entry with selective estrogen receptor modulators by disrupting the endolysosomal calcium.Scientific reports · 2017Article
- Induction of apoptosis and downregulation of ERα in DMBA-induced mammary gland tumors in Sprague-Dawley rats by synthetic 3,5-disubstituted isoxazole derivatives.Molecular and cellular biochemistry · 2016Article
- Application of virus-like particles (VLP) to NMR characterization of viral membrane protein interactions.Journal of biomolecular NMR · 2016Article
- THE STRENGTHS, WEAKNESSES, OPPORTUNITIES, AND THREATS (SWOTs) ANALYSES OF THE EBOLA VIRUS - PAPER RETRACTED.African journal of infectious diseases · 2016Article
- Crystal structure of 3-benzyl-sulfanyl-6-(5-methyl-1,2-oxazol-3-yl)-1,2,4-triazolo[3,4-b][1,3,4]thia-diazole.Acta crystallographica. Section E, Crystallographic communications · 2015Article
- Development of Small-Molecule Antivirals for Ebola.Medicinal research reviews · 2015Review
- Synthesis of Bicyclic Isoxazoles and Isoxazolines via Intramolecular Nitrile Oxide Cycloaddition.Molecules (Basel, Switzerland) · 2015Article
- Chemical and Structural Aspects of Ebola Virus Entry Inhibitors.ACS infectious diseases · 2015Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Herein, we report the development of an antifiloviral screening system, based on a pseudotyping strategy, and its application in the discovery of a novel group of small molecules that selectively inhibit the Ebola and Marburg glycoprotein (GP)-mediated infection of human cells. Using Ebola Zaire GP-pseudotyped HIV particles bearing a luciferase reporter gene and 293T cells, a library of 237 small molecules was screened for inhibition of GP-mediated viral entry. From this assay, lead compound 8a was identified as a selective inhibitor of filoviral entry with an IC(50) of 30 μM. To analyze functional group requirements for efficacy, a structure-activity relationship analysis of this 3,5-disubstituted isoxazole was then conducted with 56 isoxazole and triazole derivatives prepared using "click" chemistry. This study revealed that while the isoxazole ring can be replaced by a triazole system, the 5-(diethylamino)acetamido substituent found in 8a is required for inhibition of viral-cell entry. Variation of the 3-aryl substituent provided a number of more potent antiviral agents with IC(50) values ranging to 2.5 μM. Lead compound 8a and three of its derivatives were also found to block the Marburg glycoprotein (GP)-mediated infection of human cells.
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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.