Anti-HIV and antiplasmodial activity of original flavonoid derivatives

Bioorg Med Chem. 2010 Aug 15;18(16):6012-23. doi: 10.1016/j.bmc.2010.06.067. Epub 2010 Jun 25.

Abstract

In our search for potent anti-HIV and antiplasmodial agents, novel series of flavonoid derivatives and their chalcone intermediates were synthesized and evaluated for inhibition of HIV multiplication and antiproliferative activity on Plasmodium falciparum parasites. Chalcones exhibited a more selective antiplasmodial activity than flavonoids. Methoxyflavone 7e was the only one compound active in both P. falciparum and HIV-1 whereas aminomethoxyflavones showed activity against HIV-2. Para substitution on the B ring seemed to increase HIV-2 potency.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology*
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Cell Line
  • Cell Survival
  • Flavonoids / chemical synthesis
  • Flavonoids / chemistry*
  • Flavonoids / pharmacology*
  • HIV / drug effects
  • HIV Infections / drug therapy
  • Humans
  • Malaria, Falciparum / drug therapy
  • Plasmodium falciparum / drug effects

Substances

  • Anti-HIV Agents
  • Antimalarials
  • Flavonoids