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Synthesis and Serotonin Transporter Activity of Sulphur-substituted α-Alkyl Phenethylamines as a New Class of Anticancer Agents by Suzanne M. Cloonan; John J. Keating; Stephen G. Butler; Andrew J.S. Knox; Anne M. Jørgensen; Günther H. Peters; Dilip Rai; Desmond Corrigan; David G. Lloyd; D. Clive Williams; Mary J. Meegan is a Chemistry article available to read on EtoBox.

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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-a 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.

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Author

Suzanne M. Cloonan; John J. Keating; Stephen G. Butler; Andrew J.S. Knox; Anne M. Jørgensen; Günther H. Peters; Dilip Rai; Desmond Corrigan; David G. Lloyd; D. Clive Williams; Mary J. Meegan

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)

Published

2009

Language

EN

Field

Chemistry (Physical Sciences)