[Synthesis of thiophene and alpha-terthiophene derivatives with antiproliferative activity]

Acta Pharm Hung. 2005;75(4):185-93.
[Article in Hungarian]

Abstract

We have synthesised a series of known alpha-terthiophene lead molecules with PKC (protein kinase C) inhibitory activity and the compounds were tested in cell proliferation assay on EGF-RTK (epidermal growth factor receptor protein tyrosine kinase) over-expressing tumour cell line (A431). We found that two of them had excellent antiproliferative activity. We prepared a focused molecule library around the thiophene and the terthiophene scaffold and examined these compounds in cell proliferation assay on A431.

MeSH terms

  • Anti-Infective Agents / pharmacology*
  • Cell Division / drug effects*
  • Cell Line, Tumor
  • Enzyme Inhibitors / pharmacology
  • ErbB Receptors / antagonists & inhibitors
  • Humans
  • Protein Kinase C / antagonists & inhibitors
  • Thiophenes / pharmacology*

Substances

  • Anti-Infective Agents
  • Enzyme Inhibitors
  • Thiophenes
  • alpha-terthienyl
  • ErbB Receptors
  • Protein Kinase C