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

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 treat...

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Detalles Bibliográficos
Autores principales: Scott, Fraser J., Khalaf, Abedawn I., Giordani, Federica, Wong, Pui Ee, Duffy, Sandra, Barrett, Michael, Avery, Vicky M., Suckling, Colin J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Editions Scientifiques Elsevier 2016
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4872591/
https://www.ncbi.nlm.nih.gov/pubmed/27060763
http://dx.doi.org/10.1016/j.ejmech.2016.03.064
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author Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.
author_facet Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.
author_sort Scott, Fraser J.
collection PubMed
description 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.
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spelling pubmed-48725912016-06-30 An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics Scott, Fraser J. Khalaf, Abedawn I. Giordani, Federica Wong, Pui Ee Duffy, Sandra Barrett, Michael Avery, Vicky M. Suckling, Colin J. Eur J Med Chem Research Paper 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. Editions Scientifiques Elsevier 2016-06-30 /pmc/articles/PMC4872591/ /pubmed/27060763 http://dx.doi.org/10.1016/j.ejmech.2016.03.064 Text en © 2016 The Authors http://creativecommons.org/licenses/by/4.0/ This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Research Paper
Scott, Fraser J.
Khalaf, Abedawn I.
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M.
Suckling, Colin J.
An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
title An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
title_full An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
title_fullStr An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
title_full_unstemmed An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
title_short An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
title_sort evaluation of minor groove binders as anti-trypanosoma brucei brucei therapeutics
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4872591/
https://www.ncbi.nlm.nih.gov/pubmed/27060763
http://dx.doi.org/10.1016/j.ejmech.2016.03.064
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