1609191-04-9Relevant articles and documents
Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs
Ontoria, Jesus M.,Paonessa, Giacomo,Ponzi, Simona,Ferrigno, Federica,Nizi, Emanuela,Biancofiore, Ilaria,Malancona, Savina,Graziani, Rita,Roberts, David,Willis, Paul,Bresciani, Alberto,Gennari, Nadia,Cecchetti, Ottavia,Monteagudo, Edith,Orsale, Maria V.,Veneziano, Maria,Di Marco, Annalise,Cellucci, Antonella,Laufer, Ralph,Altamura, Sergio,Summa, Vincenzo,Harper, Steven
, p. 454 - 459 (2016/06/01)
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 50-fold). Inhibition of parasital HDACs as the mechanism of action of this new class of selective growth inhibitors is supported by hyperacetylation studies.