Potent antimalarial activity of newly synthesized substituted chalcone analogs in vitro

Several new chalcone analogues were synthesized and evaluated as inhibitors of malaria parasite. Inhibitory activity was determined in vitro against a chloroquine-sensitive Plasmodium falciparum strain of parasites. The compound 3-(4-methoxyphenyl)-1-(4-pyrrol-1-yl-phenyl)prop-2-en-1-one was found to be the most active with 50% inhibition concentration (IC(50)) of 1.61 mu g/ml. This inhibitory concentration is comparable to a prototype phytochemical chalcone, licochalcone A, with an IC(50) of 1.43 mu g/ml. The present study suggests that small, lipophilic nitrogen heterocyclic ring A together with small hydrophobic functionality at ring B can enhance antimalarial activity. These results suggest that chalcones are a class of compounds that provides an option of developing inexpensive, synthetic therapeutic antimalarial agents in the future.