Scott, F. J., Khalaf, A. I., Giordani, F. , Wong, P. E., Duffy, S., Barrett, M. , Avery, V. M. and Suckling, C. J. (2016) An evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics. European Journal of Medicinal Chemistry, 116, pp. 116-125. (doi: 10.1016/j.ejmech.2016.03.064) (PMID:27060763) (PMCID:PMC4872591)
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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.
Item Type: | Articles |
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Status: | Published |
Refereed: | Yes |
Glasgow Author(s) Enlighten ID: | Wong, Dr Pui Ee and Khalaf, Dr Abedawn and Giordani, Dr Federica and Barrett, Professor Michael |
Authors: | Scott, F. J., Khalaf, A. I., Giordani, F., Wong, P. E., Duffy, S., Barrett, M., Avery, V. M., and Suckling, C. J. |
College/School: | College of Medical Veterinary and Life Sciences > School of Infection & Immunity College of Science and Engineering > School of Chemistry |
Journal Name: | European Journal of Medicinal Chemistry |
Publisher: | Elsevier B.V. |
ISSN: | 0223-5234 |
ISSN (Online): | 1768-3254 |
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