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

Bioorganic & Medicinal Chemistry
Grazia SellittoGennaro Ciliberto

Abstract

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.

References

Sep 26, 1997·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·O ReichardO Weiland
Apr 26, 2007·Biochemistry·Eve-Isabelle PécheurStephen J Polyak

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Citations

Feb 2, 2011·PloS One·Elodie TeissierEve-Isabelle Pécheur
Apr 29, 2014·Antiviral Research·Julie BlaisingEve-Isabelle Pécheur
Aug 31, 2016·Future Medicinal Chemistry·Dmytro OstrovskyiManfred Jung
Jan 11, 2020·Acta Crystallographica. Section C, Structural Chemistry·Xue Jie TanJian Ping Ma
Aug 8, 2014·Inorganic Chemistry·Tsukasa AbeShinobu Itoh

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