Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.

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.

SUBMITTER: Ontoria JM 

PROVIDER: S-EPMC4867480 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature