Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei.


Kelly, JM; Taylor, MC; Horn, D; Loza, E; Kalvinsh, I; Björkling, F; (2012) Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei. Bioorganic & medicinal chemistry letters, 22 (5). pp. 1886-90. ISSN 0960-894X DOI: https://doi.org/10.1016/j.bmcl.2012.01.072

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Abstract

: A number of hydroxamic acid derivatives which inhibit human histone deacetylases were investigated for efficacy against cultured bloodstream form Trypanosoma brucei. Three out of the four classes tested displayed significant activity. The majority of compounds blocked parasite growth in the submicromolar range. The most potent was a member of the sulphonepiperazine series with an IC(50) of 34nM. These results identify lead compounds with potential for the development of a novel class of trypanocidal agent.

Item Type: Article
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Pathogen Molecular Biology
Research Centre: Neglected Tropical Diseases Network
PubMed ID: 22326398
Web of Science ID: 300451200009
URI: http://researchonline.lshtm.ac.uk/id/eprint/20626

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