PART I: MDMA Analogues as Lead Compounds for Burkitt’s Lymphoma Drug Discovery. PART II: Hit-to-Lead Optimisation of a Novel Class of Trypanosomacidal Agents

Stephanie Russell

Research output: ThesisDoctoral Thesis

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Abstract

This thesis describes research on two medicinal chemistry projects involving neglected diseases.
Chapter 1 discusses drug discovery for Burkitt's lymphoma (BL), centred on analogues of MDMA ('ecstasy'). Novel synthetic routes to piperonyl ketones were developed, and 15 MDMA analogues were synthesised and assessed against two BL cell lines.
The remainder of the thesis concerns drug discovery for African sleeping sickness, a parasitic disease caused by the protozoan Trypanosoma brucei. Optimisation of a high-throughput screening hit identified a novel class of N-(2-(2-phenylthiazol-4-yl)ethyl)amides, carbamates, and ureas, which rapidly and selectively kill T. brucei.100-fold increases in potency and selectivity have been achieved.

Original languageEnglish
QualificationDoctor of Philosophy
Awarding Institution
  • The University of Western Australia
Supervisors/Advisors
  • Stewart, Scott, Supervisor
  • Piggott, Matthew, Supervisor
Award date28 Oct 2016
Publication statusUnpublished - 2016

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