Synthesis and serotonin transporter activity of sulphur-substituted α-alkyl phenethylamines as a new class of anticancer agents Academic Article uri icon


MeSH Major

  • Antineoplastic Agents
  • Phenethylamines
  • Serotonin Plasma Membrane Transport Proteins
  • Sulfur


  • The discovery that some serotonin reuptake transporter (SERT) ligands have the potential to act as pro-apoptotic agents in the treatment of cancer adds greatly to their diverse pharmacological application. 4-Methylthioamphetamine (MTA) is a selective ligand for SERT over other monoamine transporters. In this study, a novel library of structurally diverse 4-MTA analogues were synthesised with or without N-alkyl and/or C-alpha methyl or ethyl groups so that their potential SERT-dependent antiproliferative activity could be assessed. Many of the compounds displayed SERT-binding activity as well as cytotoxic activity. While there was no direct correlation between these two effects, a number of derivatives displayed anti-tumour effects in lymphoma, leukaemia and breast cancer cell lines, showing further potential to be developed as possible chemotherapeutic agents.

publication date

  • December 2009



  • Academic Article



  • eng

Digital Object Identifier (DOI)

  • 10.1016/j.ejmech.2009.07.027

PubMed ID

  • 19717215

Additional Document Info

start page

  • 4862

end page

  • 88


  • 44


  • 12