title: Synthesis and antiplasmodial activity of some 1-azabenzanthrone derivatives.
abstract: 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.
authors.affiliation: Faculty of Basic Sciences, Metropolitan Educational Sciences University, Avenida J.P. Alessandri 774, Ñuñoa, Santiago 7760197, Chile. vicente.castro@umce.cl
authors.forename: Vicente
authors.initials: V
authors.lastname: Castro-Castillo
authors.forename: Cristian
authors.initials: C
authors.lastname: Suárez-Rozas
authors.forename: Adriana
authors.initials: A
authors.lastname: Pabón
authors.forename: Edwin G
authors.initials: EG
authors.lastname: Pérez
authors.forename: Bruce K
authors.initials: BK
authors.lastname: Cassels
authors.forename: Silvia
authors.initials: S
authors.lastname: Blair
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001372:Aza Compounds / Q000737:chemistry*; D001551:Benz(a)Anthracenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance / Q000187:drug effects; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D001372:Aza Compounds; D001551:Benz(a)Anthracenes; D002738:Chloroquine; C012768:benzanthrone