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Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2016 Mar 05; Vol. 7 (5), pp. 454-9. Date of Electronic Publication: 2016 Mar 05 (Print Publication: 2016). - Publication Year :
- 2016
-
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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 7
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 27190592
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.5b00468