Some synthetic 1-azabenzanthrones (7H-dibenzo[de,h]quinolin-7-ones) are weakly to moderately cytotoxic,
suggesting that they might also show antiparasitic activity. We have now tested a small collection
of these compounds in vitro against a chloroquine-resistant Plasmodium falciparum strain, comparing
their cytotoxicity against normal human fibroblasts. Our results indicate that 5-methoxy-1-azabenzanthrone
and its 2,3-dihydro analogue have low micromolar antiplasmodial activities and showed more
than 10-fold selectivity against the parasite, indicating that the dihydro compound, in particular, might
serve as a lead compound for further development.