Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.
ACS Med Chem Lett
; 7(5): 454-9, 2016 May 12.
Article
em En
| MEDLINE
| ID: mdl-27190592
ABSTRACT
The identification of a new series of P. falciparum growth inhibitors is described. Starting from a series of known human class I HDAC inhibitors a SAR exploration based on growth inhibitory activity in parasite and human cells-based assays led to the identification of compounds with submicromolar inhibition of P. falciparum growth (EC50 < 500 nM) and good selectivity over the activity of human HDAC in cells (up to >50-fold). Inhibition of parasital HDACs as the mechanism of action of this new class of selective growth inhibitors is supported by hyperacetylation studies.
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MEDLINE
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En
Ano de publicação:
2016
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Article