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

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

doi:10.1016/j.ejmech.2016.03.064

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

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

Pure And Applied Chemistry

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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.

Original language	English
Pages (from-to)	116-125
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	116
Early online date	29 Mar 2016
DOIs	https://doi.org/10.1016/j.ejmech.2016.03.064
Publication status	Published - 30 Jun 2016

Keywords

minor groove binders
antiparasitic activity
african trypanosmiasis

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10.1016/j.ejmech.2016.03.064Licence: CC BY 4.0

Scott-etal-EJMECH-2016-An-evaluation-of-minor-groove-binders-as-anti-trypanosma-bruceiFinal published version, 557 KBLicence: CC BY 4.0

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title = "An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics",

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.",

keywords = "minor groove binders, antiparasitic activity, african trypanosmiasis",

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T1 - An evaluation of minor groove binders as anti-Trypanosoma brucei brucei therapeutics

AU - Scott, Fraser J.

AU - Khalaf, Abedawn I.

AU - Giordani, Federica

AU - Wong, Pui Ee

AU - Duffy, Sandra

AU - Barrett, Michael

AU - Avery, Vicky M.

AU - Suckling, Colin J.

PY - 2016/6/30

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N2 - 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.

AB - 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.

KW - minor groove binders

KW - antiparasitic activity

KW - african trypanosmiasis

UR - http://www.sciencedirect.com/science/article/pii/S0223523416302471

U2 - 10.1016/j.ejmech.2016.03.064

DO - 10.1016/j.ejmech.2016.03.064

M3 - Article

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EP - 125

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

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

Abstract

Keywords

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