Amino acid derivatives. Part I. Synthesis, antiviral and antitumor evaluation of new alpha-amino acid esters bearing coumarin side chain

Acta Pharm. 2006 Jun;56(2):175-88.

Abstract

A series of amino acid esters bearing coumarin (3-15) were synthesized and evaluated, in vitro, against HIV-1, and bovine viral diarrhea virus (BVDV). The in vitro cytotoxicity of 3-10 and 12 was assayed against a panel of tumor cell lines consisting of CD4 human T-cells. Compound 14 showed inhibition of HIV-1 with EC50 > 1.6 microg mL(-1), meanwhile compound 9 exhibited activity against leukaemia (MT4) with CC50 = 24 micromol L(-1).

Publication types

  • Comparative Study

MeSH terms

  • Amino Acids / chemical synthesis
  • Amino Acids / pharmacology*
  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Coumarins / chemical synthesis
  • Coumarins / pharmacology*
  • Diarrhea Viruses, Bovine Viral / drug effects*
  • Diarrhea Viruses, Bovine Viral / growth & development
  • Esters
  • HIV-1 / drug effects*
  • HIV-1 / growth & development
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Amino Acids
  • Antineoplastic Agents
  • Antiviral Agents
  • Coumarins
  • Esters