Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593734 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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 IC50 of 34Â nM. These results identify lead compounds with potential for the development of a novel class of trypanocidal agent.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
John M. Kelly, Martin C. Taylor, David Horn, Einars Loza, Ivars Kalvinsh, Fredrik Björkling,