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

Scott, F. J., Khalaf, A. I., Giordani, F. , Wong, P. E., Duffy, S., Barrett, M. , Avery, V. M. and Suckling, C. J. (2016) An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics. European Journal of Medicinal Chemistry, 116, pp. 116-125. (doi:10.1016/j.ejmech.2016.03.064) (PMID:27060763) (PMCID:PMC4872591)

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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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Giordani, Dr Federica and Barrett, Professor Michael and Wong, Dr Pui Ee and Khalaf, Dr Abedawn
Authors: Scott, F. J., Khalaf, A. I., Giordani, F., Wong, P. E., Duffy, S., Barrett, M., Avery, V. M., and Suckling, C. J.
College/School:College of Medical Veterinary and Life Sciences > Institute of Infection Immunity and Inflammation
College of Science and Engineering > School of Chemistry
Journal Name:European Journal of Medicinal Chemistry
Publisher:Elsevier B.V.
ISSN:0223-5234
ISSN (Online):1768-3254

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Project CodeAward NoProject NamePrincipal InvestigatorFunder's NameFunder RefLead Dept
466861Conditional translational repression: a core regulatory mechanism of gene expression during development of the malaria parasite.Andrew WatersWellcome Trust (WELLCOME)083811/Z/07/ZIII - PARASITOLOGY