An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics
Author(s)
Scott, Fraser J
Khalaf, Abedawn I
Giordani, Federica
Wong, Pui Ee
Duffy, Sandra
Barrett, Michael
Avery, Vicky M
Suckling, Colin J
Year published
2016
Metadata
Show full item recordAbstract
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.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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Journal Title
European Journal of Medicinal Chemistry
Volume
116
Subject
Medicinal and biomolecular chemistry
Medicinal and biomolecular chemistry not elsewhere classified
Organic chemistry
Pharmacology and pharmaceutical sciences