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

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Authors

Gandy, Michael N
McIldowie, Matthew
Lewis, Katie
Wasik, Agata M
Salomonczyk, Danielle
Wagg, Keith
Millar, Zak A
Tindiglia, David
Huot, Philippe
Johnston, Tom

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Royal Society of Chemistry

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.

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MedChemComm

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Restricted until

2037-12-31