An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics

Eur J Med Chem. 2016 Jun 30:116:116-125. doi: 10.1016/j.ejmech.2016.03.064.

Fraser J Scott ¹, Abedawn I Khalaf ², Federica Giordani ³, Pui Ee Wong ³, Sandra Duffy ⁴, Michael Barrett ³, Vicky M Avery ⁴, Colin J Suckling ²

Affiliations

1 WestCHEM Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom. Electronic address: fraser.j.scott@strath.ac.uk.
2 WestCHEM Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom.
3 Wellcome Trust Centre for Molecular Parasitology, Institute of Infection, Immunity and Inflammation and Glasgow Polyomics, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8TA, United Kingdom.
4 Discovery Biology, Eskitis Institute for Drug Discovery, Griffith University, Nathan, Queensland 4111, Australia.

PMID: 27060763 DOI: 10.1016/j.ejmech.2016.03.064

Abstract

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.

Keywords

African trypanosomiasis; Antiparasitic activity; Minor Groove Binders.

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