Issue 4, 2010
From the journal:

MedChemComm

Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt's lymphoma cytotoxicity†

Michael N. Gandy,a   Matthew McIldowie,a   Katie Lewis,a   Agata M. Wasik,b   Danielle Salomonczyk,c   Keith Wagg,d   Zak A. Millar,e   David Tindiglia,e   Philippe Huot,f   Tom Johnston,f   Sherri Thiele,f   Blake Nguyen,a   Nicholas M. Barnes,g   Jonathan M. Brotchie,f   Mathew T. Martin-Iverson,e   Joanne Nash,c   John Gordonb  and  Matthew J. Piggott*a  

* Corresponding authors

a School of Biomedical, Biomolecular and Chemical Sciences, The University of Western Australia, Crawley, WA, Australia
E-mail: piggott@cyllene.uwa.edu.au
Fax: +61 6488 1005
Tel: +61 6488 3170

b MRC Centre for Immune Regulation, The Medical School, University of Birmingham, UK

c Centre for Neurobiology of Stress, Department of Biological Sciences, University of Toronto at Scarborough, 1265 Military Trail, Toronto, ON, Canada

d Department of Chemistry, The Australian National University, Canberra, ACT, Australia

e School of Medicine and Pharmacology, The University of Western Australia, Crawley, WA, Australia

f Toronto Western Research Institute, Toronto Western Hospital, 399 Bathurst Street, MC 11-419, Toronto, ON, Canada

g Clinical and Experimental Medicine, The Medical School, University of Birmingham, UK

Abstract

Burkitt's lymphoma (BL) is a particularly aggressive cancer that primarily affects African children. Unfortunately, effective and affordable treatment is out of reach of most of the afflicted. The illicit psychoactive drug methylenedioxymethamphetamine (MDMA, ‘ecstasy’) is cytotoxic to BL cell lines, but its low potency, psychoactivity and neurotoxicity preclude consideration as a therapeutic drug candidate. This paper describes the discovery of novel α-aryl analogues of MDMA that lack psychoactivity and reduce BL cell line viability with significantly more potency than the lead compound. Preliminary in vitro studies also indicate that the compounds are non-toxic to a relevant neuronal cell line.

Graphical abstract: Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt's lymphoma cytotoxicity

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Article information

DOI
https://doi.org/10.1039/C0MD00108B
Article type
Concise Article
Submitted
12 Jul 2010
Accepted
30 Jul 2010
First published
07 Sep 2010

Med. Chem. Commun., 2010,1, 287-293

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Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt's lymphoma cytotoxicity

M. N. Gandy, M. McIldowie, K. Lewis, A. M. Wasik, D. Salomonczyk, K. Wagg, Z. A. Millar, D. Tindiglia, P. Huot, T. Johnston, S. Thiele, B. Nguyen, N. M. Barnes, J. M. Brotchie, M. T. Martin-Iverson, J. Nash, J. Gordon and M. J. Piggott, Med. Chem. Commun., 2010, 1, 287 DOI: 10.1039/C0MD00108B

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