Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 7, Issue 5, Pages 454-459Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00468
Keywords
Malaria; Plasmodium falciparum; PfHDAC1; 4-arylimidazoles
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Funding
- Medicine for Malaria Venture (MMV)
- National Collection of Compounds and Chemical Screening Center (CNCCS Consortium)
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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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