Discovery of Pyrano[3,4-b]indoles as Potent and Selective HCV NS5B Polymerase Inhibitors

A novel series of HCV NS5B RNA-dependent RNA polymerase inhibitors containing a pyrano[3,4-b]indole scaffold is described leading to the discovery of compound 16, a highly potent and selective inhibitor that is active in the replicon system.

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Veröffentlicht in:Journal of medicinal chemistry 2004-12, Vol.47 (26), p.6603-6608
Hauptverfasser: Gopalsamy, Ariamala, Lim, Kitae, Ciszewski, Gregory, Park, Kaapjoo, Ellingboe, John W, Bloom, Jonathan, Insaf, Shabana, Upeslacis, Janis, Mansour, Tarek S, Krishnamurthy, Girija, Damarla, Murthy, Pyatski, Yelena, Ho, Douglas, Howe, Anita Y. M, Orlowski, Mark, Feld, Boris, O'Connell, John
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container_end_page 6608
container_issue 26
container_start_page 6603
container_title Journal of medicinal chemistry
container_volume 47
creator Gopalsamy, Ariamala
Lim, Kitae
Ciszewski, Gregory
Park, Kaapjoo
Ellingboe, John W
Bloom, Jonathan
Insaf, Shabana
Upeslacis, Janis
Mansour, Tarek S
Krishnamurthy, Girija
Damarla, Murthy
Pyatski, Yelena
Ho, Douglas
Howe, Anita Y. M
Orlowski, Mark
Feld, Boris
O'Connell, John
description A novel series of HCV NS5B RNA-dependent RNA polymerase inhibitors containing a pyrano[3,4-b]indole scaffold is described leading to the discovery of compound 16, a highly potent and selective inhibitor that is active in the replicon system.
doi_str_mv 10.1021/jm0401255
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subjects Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Biological and medical sciences
Crystallography, X-Ray
DNA-Directed RNA Polymerases - antagonists & inhibitors
DNA-Directed RNA Polymerases - chemistry
Hepacivirus - enzymology
Hepatitis C virus
Indoles - chemical synthesis
Indoles - chemistry
Medical sciences
Pharmacology. Drug treatments
Pyrans - chemical synthesis
Pyrans - chemistry
Stereoisomerism
Structure-Activity Relationship
Viral Nonstructural Proteins - antagonists & inhibitors
Viral Nonstructural Proteins - chemistry
title Discovery of Pyrano[3,4-b]indoles as Potent and Selective HCV NS5B Polymerase Inhibitors
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