4-Phenylcoumarins as HIV transcription inhibitors

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4447-50. doi: 10.1016/j.bmcl.2005.07.041.


We have evaluated the anti-HIV activity of eleven natural 4-phenylcoumarins isolated from Marila pluricostata and three of their derivatives. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase gene as reporter. Inhibitions of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Most of the coumarins tested displayed NF-kappaB inhibition. Two coumarins were also Tat antagonists and the presence of both activities correlated with a stronger inhibition of HIV replication. Our results show that antiviral effect of 4-phenylcoumarins can be related to the inhibition of NF-kappaB and Tat, and suggest that these types of compounds can be useful in the treatment of HIV infection as viral transcription inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Gene Products, tat / antagonists & inhibitors
  • HIV / drug effects*
  • HIV / genetics
  • HIV / physiology
  • HeLa Cells
  • Humans
  • NF-kappa B / antagonists & inhibitors
  • Transcription, Genetic / drug effects*
  • Virus Replication
  • tat Gene Products, Human Immunodeficiency Virus


  • Anti-HIV Agents
  • Coumarins
  • Gene Products, tat
  • NF-kappa B
  • tat Gene Products, Human Immunodeficiency Virus
  • 4-phenylcoumarin