Synthesis and HIV-1 integrase inhibitory activities of caffeic acid dimers derived from Salvia officinalis

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5053-6. doi: 10.1016/j.bmcl.2005.07.091. Epub 2005 Sep 23.

Abstract

The synthesis of two caffeoyl-coumarin conjugates, derived from sagecoumarin, has been accomplished, starting from ferulic acid, isoferulic acid and sesamol. Both compounds exhibited potent inhibitory activities at micromolar concentrations against HIV-1 integrase in 3'-end processing reaction but were less effective against HIV-1 replication in a single-round infection assay of HeLa-beta-gal-CD4+ cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Caffeic Acids / chemical synthesis*
  • Caffeic Acids / chemistry
  • Caffeic Acids / isolation & purification
  • Caffeic Acids / pharmacology*
  • Coumarins / chemistry
  • Dimerization
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / chemical synthesis*
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / isolation & purification
  • HIV Integrase Inhibitors / pharmacology*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Salvia officinalis / chemistry*

Substances

  • Caffeic Acids
  • Coumarins
  • HIV Integrase Inhibitors
  • coumarin
  • HIV Integrase