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

TY - JOUR

T1 - Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei

AU - Kelly, John

AU - Taylor, M C

AU - Horn, David

AU - Loza, Einars

AU - Kalvinsh, Ivars

AU - Björkling, Fredrik

PY - 2012/3/1

Y1 - 2012/3/1

N2 - 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.

AB - 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.

U2 - 10.1016/j.bmcl.2012.01.072

DO - 10.1016/j.bmcl.2012.01.072

M3 - Journal article

C2 - 22326398

SN - 0960-894X

VL - 22

SP - 1886

EP - 1890

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 5

ER -