Synthesis, antiviral and antiproliferative activity of a new class of 5-(alkyl or arylthio)-6-vinyl uracils

Anticancer Drug Des. 1996 Dec;11(8):597-609.

Abstract

Uracil derivatives bearing substituted or unsubstituted vinyl groups at position C6 and alkyl- or arylthio groups at position C5 were synthesized and tested in vitro for antiviral and antiproliferative activity. None of the compounds were active against HIV-1. However, some of them inhibited the proliferation of leukemia, lymphoma and solid tumor-derived cell lines at micromolar concentrations. The maximum potency of antiproliferative activity correlates with the presence of unsubstituted vinyl groups and alkyl- or arylthio substituents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Division / drug effects
  • Drug Screening Assays, Antitumor
  • HIV-1 / drug effects
  • Humans
  • Thionucleotides / chemical synthesis*
  • Thionucleotides / pharmacology
  • Tumor Cells, Cultured
  • Uracil / analogs & derivatives*
  • Uracil / chemical synthesis
  • Uracil / pharmacology
  • Vinyl Compounds / chemical synthesis*
  • Vinyl Compounds / pharmacology

Substances

  • Anti-HIV Agents
  • Antineoplastic Agents
  • Thionucleotides
  • Vinyl Compounds
  • Uracil