Lycorine-derived phenanthridine downregulators of host Hsc70 as potential hepatitis C virus inhibitors

Future Med Chem. 2015;7(5):561-70. doi: 10.4155/fmc.15.14.

Abstract

Background: A new series of potential phenanthridine hepatitis C virus (HCV) inhibitors which work by suppressing Hsc70 expression in the host cell was designed and synthesized from lycorine.

Results: Thirty-one new potential phenanthridine HCV inhibitors were synthesized and five of these compounds exhibited good anti-HCV activity and these inhibitors probably inhibit HCV by downregulating the host Hsc70 expression. Structure-activity analysis of these compounds revealed that the double bond between C-11 and C-12 and the substituents at C-8 and C-9 are important for their activity against HCV.

Conclusion: Suppression of Hsc70 expression in the host cell to limit HCV replication is a potential anti-HCV strategy. Phenanthridines are probably the HCV inhibitors with this mode of action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amaryllidaceae Alkaloids / chemistry*
  • Amaryllidaceae Alkaloids / pharmacology*
  • Antiviral Agents / chemistry*
  • Antiviral Agents / pharmacology*
  • Cell Line
  • Down-Regulation / drug effects
  • HSC70 Heat-Shock Proteins / genetics*
  • Hepacivirus / drug effects*
  • Hepacivirus / physiology
  • Hepatitis C / drug therapy*
  • Hepatitis C / genetics
  • Hepatocytes / drug effects
  • Hepatocytes / metabolism
  • Hepatocytes / virology
  • Humans
  • Phenanthridines / chemistry*
  • Phenanthridines / pharmacology*
  • Virus Replication / drug effects

Substances

  • Amaryllidaceae Alkaloids
  • Antiviral Agents
  • HSC70 Heat-Shock Proteins
  • Phenanthridines
  • lycorine