An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics

Scott, Fraser J. and Khalaf, Abedawn I. and Giordani, Federica and Wong, Pui Ee and Duffy, Sandra and Barrett, Michael and Avery, Vicky M. and Suckling, Colin J. (2016) An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics. European Journal of Medicinal Chemistry, 116. pp. 116-125. ISSN 0223-5234 (https://doi.org/10.1016/j.ejmech.2016.03.064)

[thumbnail of Scott-etal-EJMECH-2016-An-evaluation-of-minor-groove-binders-as-anti-trypanosma-brucei]
Preview
 Text. Filename: Scott_etal_EJMECH_2016_An_evaluation_of_minor_groove_binders_as_anti_trypanosma_brucei.pdf
Final Published Version
License: Creative Commons Attribution 4.0 logo
Download (570kB)| Preview

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.

CORE (COnnecting REpositories)