Potent inhibitors of hepatitis C core dimerization as new leads for anti-hepatitis C agents

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2198-202. doi: 10.1016/j.bmcl.2011.03.014.

Abstract

New indoline alkaloid-type compounds which inhibit HCV production by infected hepatoma cells have been identified. These compounds, dimeric-type compounds of previously known inhibitors, display double digit nanomolar IC(50) and EC(50) values, with cytotoxicity CC(50) indexes higher than 36 μM, thus providing ample therapeutic windows for further development of HCV drugs.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Alkaloids / chemical synthesis
  • Alkaloids / chemistry
  • Alkaloids / toxicity
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry*
  • Antiviral Agents / toxicity
  • Cell Line, Tumor
  • Dimerization
  • Hepacivirus / drug effects*
  • Hepacivirus / metabolism
  • Humans
  • Indoles / chemistry
  • Viral Core Proteins / antagonists & inhibitors*
  • Viral Core Proteins / metabolism

Substances

  • Alkaloids
  • Antiviral Agents
  • Indoles
  • Viral Core Proteins
  • nucleocapsid protein, Hepatitis C virus
  • indoline