Antimalarial activity of ferrocenyl chalcones.
A series of ferrocenyl chalcones were synthesized and evaluated for in vitro antimalarial activity against a chloroquine-resistant strain of Plasmodium falciparum. The most active compounds were 1-(3-pyridyl)-3-ferrocenyl-2-propen-1-one (6) and 1-ferrocenyl-3-(4-nitrophenyl)-2-propen-1-one (28) with IC(50) of 4.5 and 5.1 microM, respectively. Differences in activity were not readily explained by the size and lipophilicity characteristics of these compounds.
Wu
Xiang
X
Department of Pharmacy, National University of Singapore, 18, Science Drive 4, Singapore 117543, Singapore.
Wilairat
Prapon
P
Go
Mei-Lin
ML
D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology; D002599:Chalcone / Q000737:chemistry* / Q000494:pharmacology; D002738:Chloroquine; D004351:Drug Resistance; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology; D019271:Hypoxanthine / Q000037:antagonists & inhibitors / Q000493:pharmacokinetics; D020128:Inhibitory Concentration 50; D000075163:Metallocenes; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
D000962:Antimalarials; D005296:Ferrous Compounds; D000075163:Metallocenes; D019271:Hypoxanthine; D002599:Chalcone; D002738:Chloroquine; C004998:ferrocene