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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. 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

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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

Item Type: Article
Subjects: Q Science > QD Chemistry
Schools: School of Applied Sciences
Depositing User: Fraser Scott
Date Deposited: 15 Aug 2017 09:32
Last Modified: 28 Aug 2021 15:44


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