Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4416-9. doi: 10.1016/j.bmcl.2010.06.052. Epub 2010 Jun 12.

Abstract

A series of beta-carboline derivatives were synthesized by utilizing aromatization and chemoselective alkylation method recently reported from our laboratory. Synthesized derivatives were evaluated for anti-HIV activity in human CD4+ T cell line (CEM-GFP) infected with HIV-1 NL(4.3) virus. 1-Formyl-beta-carboline-3-carbxylic acid methyl ester (15) showed inhibition of human immunodeficiency virus at IC(50)=2.9 microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Carbolines / chemical synthesis
  • Carbolines / chemistry*
  • Carbolines / pharmacology
  • Cell Line
  • Formates / chemical synthesis*
  • Formates / chemistry
  • Formates / pharmacology
  • HIV / drug effects*
  • Humans

Substances

  • 1-formyl-beta-carboline-3-carbxylic acid methyl ester
  • Anti-HIV Agents
  • Carbolines
  • Formates