Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro

Grazia Sellitto, Aurora Faruolo, Paolo De Caprariis, Sergio Altamura, Giacomo Paonessa, Gennaro Ciliberto

Research output: Contribution to journalArticle

Abstract

A series of ethyl 1H-indole-3-carboxylates 9a1- 6 and 9b1-2 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 9a2 (>10; >16.7) and 9b1 (>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 9a3 (>6.25) was higher than that of ARB (6). Of these three initial hits, compound 9a2 was the most potent.

Original languageEnglish
Pages (from-to)6143-6148
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number16
DOIs
Publication statusPublished - Aug 15 2010

Keywords

  • Arbidol
  • Ethyl 1H-indole-3-carboxylates
  • Hepatitis C virus
  • Synthesis

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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