Synthesis and antiplasmodial activity of some 1-azabenzanthrone derivatives
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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.
Artículo de publicación ISI
DOI: DOI: 10.1016/j.bmcl.2012.10.092
Quote ItemBioorganic & Medicinal Chemistry Letters 23 (2013) 327–329