Document Detail


Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro.
MedLine Citation:
PMID:  20638289     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A series of ethyl 1H-indole-3-carboxylates 9a(1)(-)(6) and 9b(1)(-)(2) were prepared and evaluated in Huh-7.5 cells. Most of the compounds exhibited anti-hepatitis C virus (HCV) activities at low concentration. The selectivity indices of inhibition on entry and replication of compounds 9a(2) (>10; >16.7) and 9b(1) (>6.25; >16.7) were higher than those of the other evaluated compounds, including the lead compound Arbidol (ARB, 6; 15). Moreover, the selective index of inhibition on entry of compound 9a(3) (>6.25) was higher than that of ARB (6). Of these three initial hits, compound 9a(2) was the most potent.
Authors:
Grazia Sellitto; Aurora Faruolo; Paolo de Caprariis; Sergio Altamura; Giacomo Paonessa; Gennaro Ciliberto
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Publication Detail:
Type:  Comparative Study; Journal Article     Date:  2010-06-22
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-08-09     Completed Date:  2010-12-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  6143-8     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Dipartimento di Scienze Farmaceutiche,Università di Salerno, Fisciano, Italy. gsellitto@unisa.it
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MeSH Terms
Descriptor/Qualifier:
Antiviral Agents / chemical synthesis,  chemistry*,  pharmacology*
Carboxylic Acids / chemical synthesis,  chemistry,  pharmacology
Cell Line
Hepacivirus / drug effects*
Hepatitis C / drug therapy
Humans
Indoles / chemical synthesis,  chemistry*,  pharmacology*
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Antiviral Agents; 0/Carboxylic Acids; 0/Indoles; 131707-23-8/arbidol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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