Tryptamine derivatives as novel non-nucleosidic inhibitors against hepatitis B virus

Bioorg Med Chem. 2011 May 15;19(10):3120-7. doi: 10.1016/j.bmc.2011.04.004. Epub 2011 Apr 6.

Abstract

A series of tryptamine derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compounds 2e and 4a showed potent antiviral activity (IC(50)=0.4 and <1 μM, respectively) and low cytotoxicity (CC(50)=40.6 and >25 μM, respectively).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemistry*
  • Antiviral Agents / pharmacology*
  • Cell Survival / drug effects
  • DNA, Viral / metabolism
  • Hep G2 Cells
  • Hepatitis B / drug therapy*
  • Hepatitis B virus / drug effects*
  • Humans
  • Structure-Activity Relationship
  • Tryptamines / chemistry*
  • Tryptamines / pharmacology*

Substances

  • Antiviral Agents
  • DNA, Viral
  • Tryptamines
  • tryptamine