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

Research output: Contribution to journalArticle

12 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

Fingerprint

African Trypanosomiasis
Trypanosoma brucei brucei
Bioactivity
Biological Products
Modulators
Binders
Animals
Therapeutics
stallimycin

Cite this

Scott, F. J., Khalaf, A. I., Giordani, F., Wong, P. E., Duffy, S., Barrett, 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
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. In: European Journal of Medicinal Chemistry. 2016 ; Vol. 116. pp. 116-125.
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Scott, FJ, Khalaf, AI, Giordani, F, Wong, PE, Duffy, S, Barrett, M, Avery, VM & Suckling, CJ 2016, 'An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics', European Journal of Medicinal Chemistry, vol. 116, pp. 116-125. https://doi.org/10.1016/j.ejmech.2016.03.064

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.

In: European Journal of Medicinal Chemistry, Vol. 116, 30.06.2016, p. 116-125.

Research output: Contribution to journalArticle

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