Synthesis and in vitro anti-hepatitis B virus activities of some ethyl 5-hydroxy-1H-indole-3-carboxylates

Bioorg Med Chem. 2006 Apr 15;14(8):2552-8. doi: 10.1016/j.bmc.2005.11.033. Epub 2005 Dec 1.

Abstract

A series of ethyl 5-hydroxy-1H-indole-3-carboxylates 6A-10T were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC50 and selective index of inhibition on replication of HBV DNA of compounds 10(L) (1.52 microg/ml, 9.38) and 10(P) (2.00 microg/ml, 8.85) were higher than those of the other evaluated compounds including lamivudine (7.02). Compounds 7E and 10J exhibited significant anti-HBV activities, and the IC50 values on replication of HBV DNA of these compounds were 24.90 and 15.41 microg/ml, respectively, which were far more potent than the positive control lamivudine 228.00 microg/ml.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology*
  • Cell Line
  • DNA Replication / drug effects
  • Hepatitis B virus / drug effects*
  • Hepatitis B virus / genetics
  • Indoles / chemical synthesis*
  • Indoles / pharmacology*
  • Spectrometry, Mass, Electrospray Ionization

Substances

  • Antiviral Agents
  • Indoles