Synthesis and in-vitro anti-hepatitis-B virus activity of 6H-[1]benzothiopyrano[4,3-b] quinolin-10-ols

Arch Pharm (Weinheim). 2009 Sep;342(9):507-12. doi: 10.1002/ardp.200900070.

Abstract

A series of 9-methoxy-6H-[1]benzothiopyrano[4,3-b]quinolin-10-ols with a Mannich side chain were synthesized and evaluated for their anti-Hepatitis B virus (HBV) activity in HepG2.2.15 cells. Some compounds showed significant anti-HBV activity with IC(50) values less than 41 microM. Among them, compound 9b was the most effective anti-HBV agent (IC(50) = 1.7 microM, SI = 60.3).

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Cell Line
  • Cell Survival / drug effects*
  • DNA, Viral / metabolism
  • Drug Evaluation, Preclinical
  • Drug Resistance, Viral
  • Hepatitis B virus / drug effects*
  • Hepatitis B virus / metabolism
  • Hydroxyquinolines / pharmacology*
  • Lamivudine / pharmacology
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • DNA, Viral
  • Hydroxyquinolines
  • Lamivudine