Synthesis and antiplasmodial activity of some 1-azabenzanthrone derivatives |
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| Authors: | Vicente Castro-Castillo Cristian Suárez-Rozas Adriana Pabón Edwin G Pérez Bruce K Cassels Silvia Blair |
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| Institution: | 1. Faculty of Basic Sciences, Metropolitan Educational Sciences University, Avenida J.P. Alessandri 774, Ñuñoa, Santiago 7760197, Chile;2. Grupo Malaria, Universidad de Antioquia, Calle 67, 53-108 Medellín, Colombia;3. Facultad de Química, Pontificia Universidad Católica de Chile, Av. Vicuña Mackenna 4860, Santiago 6094411, Chile;4. Department of Chemistry, Faculty of Sciences, University of Chile, Las Palmeras 3425, Ñuñoa, Santiago 7800024, Chile |
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| Abstract: | Some synthetic 1-azabenzanthrones (7H-dibenzode,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. |
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