Plasmepsin II inhibitory activity of alkoxylated and hydroxylated chalcones.

Sixteen antimalarial alkoxylated and hydroxylated chalcones were tested for their ability to inhibit recombinant plasmepsin II in vitro. The best inhibitory compounds had either a chloro or dimethylamino group at the 4-position of phenyl ring A in the chalcone template. Combination of the chalcones with chloroquine showed additivity or mild antagonism of Plasmodium falciparum K1 growth in culture.