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

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

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14 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)116-125
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume116
Early online date29 Mar 2016
DOIs
Publication statusPublished - 30 Jun 2016
Externally publishedYes

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  • Cite this

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