title: Plasmepsin II inhibitory activity of alkoxylated and hydroxylated chalcones.
abstract: 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.
authors.affiliation: Department of Biochemistry, Faculty of Science, Mahidol University, Bangkok, Thailand.
authors.forename: Nongluk
authors.initials: N
authors.lastname: Sriwilaijaroen
authors.forename: Mei
authors.initials: M
authors.lastname: Liu
authors.forename: Mei-Lin
authors.initials: ML
authors.lastname: Go
authors.forename: Prapon
authors.initials: P
authors.lastname: Wilairat
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002738:Chloroquine / Q000633:toxicity*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects*; D015800:Protozoan Proteins
chemical_list: D000962:Antimalarials; D047188:Chalcones; D015800:Protozoan Proteins; D002738:Chloroquine; D016282:Aspartic Acid Endopeptidases; C100637:plasmepsin II