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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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

Information

URI:

https://eprints.hud.ac.uk/id/eprint/32649

Title:

An evaluation of Minor Groove Binders as anti- Trypanosoma brucei brucei therapeutics

Creators:

Scott, Fraser J., Khalaf, Abedawn I., Giordani, Federica, Wong, Pui Ee, Duffy, Sandra, Barrett, Michael, Avery, Vicky M. and Suckling, Colin J.

Identification Number:

10.1016/j.ejmech.2016.03.064

Official URL:

https://doi.org/10.1016/j.ejmech.2016.03.064

Date:

30 June 2016

Subjects:

Q Science > QD Chemistry

Schools:

School of Applied Sciences

Library

Item Type:

Article

Depositing User:

Fraser Scott

Date Deposited:

15 Aug 2017 09:32

Revision:

Last Modified:

28 Aug 2021 15:44

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