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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:
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
Descripción
Sumario: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.