Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.
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Cloonan SM, Keating JJ, Butler SG, Knox AJ, Jorgensen AM, Peters GH, Rai D, Corrigan D, Lloyd DG, Williams DC, Meegan MJ
Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.
Eur J Med Chem. 2009 Dec;44(12):4862-88. doi: 10.1016/j.ejmech.2009.07.027. Epub 2009 Aug 6.
- PubMed ID
- 19717215 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Midomafetamine Sodium-dependent dopamine transporter IC 50 (nM) 1442 N/A N/A Details Midomafetamine Sodium-dependent noradrenaline transporter IC 50 (nM) 405 N/A N/A Details Midomafetamine Sodium-dependent serotonin transporter IC 50 (nM) 425 N/A N/A Details