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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.

SUBMITTER: Scott FJ

PROVIDER: S-EPMC4872591 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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

Scott Fraser J FJ Khalaf Abedawn I AI Giordani Federica F Wong Pui Ee PE Duffy Sandra S Barrett Michael M Avery Vicky M VM Suckling Colin J CJ

European journal of medicinal chemistry 20160329

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. ...[more]

PMID: 27060763

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