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

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 submicro...

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Autores principales: Kelly, John M., Taylor, Martin C., Horn, David, Loza, Einars, Kalvinsh, Ivars, Björkling, Fredrik
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Science Ltd 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3314994/
https://www.ncbi.nlm.nih.gov/pubmed/22326398
http://dx.doi.org/10.1016/j.bmcl.2012.01.072
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author Kelly, John M.
Taylor, Martin C.
Horn, David
Loza, Einars
Kalvinsh, Ivars
Björkling, Fredrik
author_facet Kelly, John M.
Taylor, Martin C.
Horn, David
Loza, Einars
Kalvinsh, Ivars
Björkling, Fredrik
author_sort Kelly, John M.
collection PubMed
description 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 34 nM. These results identify lead compounds with potential for the development of a novel class of trypanocidal agent.
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spelling pubmed-33149942012-04-11 Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei Kelly, John M. Taylor, Martin C. Horn, David Loza, Einars Kalvinsh, Ivars Björkling, Fredrik Bioorg Med Chem Lett Article 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 34 nM. These results identify lead compounds with potential for the development of a novel class of trypanocidal agent. Elsevier Science Ltd 2012-03-01 /pmc/articles/PMC3314994/ /pubmed/22326398 http://dx.doi.org/10.1016/j.bmcl.2012.01.072 Text en © 2012 Elsevier Ltd. https://creativecommons.org/licenses/by/3.0/ Open Access under CC BY 3.0 (https://creativecommons.org/licenses/by/3.0/) license
spellingShingle Article
Kelly, John M.
Taylor, Martin C.
Horn, David
Loza, Einars
Kalvinsh, Ivars
Björkling, Fredrik
Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
title Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
title_full Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
title_fullStr Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
title_full_unstemmed Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
title_short Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
title_sort inhibitors of human histone deacetylase with potent activity against the african trypanosome trypanosoma brucei
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3314994/
https://www.ncbi.nlm.nih.gov/pubmed/22326398
http://dx.doi.org/10.1016/j.bmcl.2012.01.072
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