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

John M. Kelly, Martin C. Taylor, David Horn, Einars Loza, Ivars Kalvinsh, Fredrik Bjorkling

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    18 Citations (Scopus)

    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 34 nM. These results identify lead compounds with potential for the development of a novel class of trypanocidal agent. (c) 2012 Elsevier Ltd. All rights reserved.

    Original languageEnglish
    Pages (from-to)1886-1890
    Number of pages5
    JournalBioorganic & Medicinal Chemistry Letters
    Volume22
    Issue number5
    DOIs
    Publication statusPublished - 1 Mar 2012

    Keywords

    • SLEEPING SICKNESS
    • Histone deacetylase inhibitors
    • MARK
    • SELECTIVITY
    • Hydroxamic acids
    • Anti-parasitic activity
    • CYCLE
    • ANTIMALARIAL
    • Trypanosoma brucei

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