2013 |
Castro-Castillo, V; Suarez-Rozas, C; Pabon, A; Perez, E G; Cassels, B K; Blair, S Synthesis and Antiplasmodial Activity of Some 1-Azabenzanthrone Derivatives Artículo de revista Bioorganic & Medicinal Chemistry Letters, 23 (1), pp. 327-329, 2013, ISSN: 0960-894x. Resumen | Enlaces | BibTeX | Etiquetas: alkaloids antimalarial, chloroquine-resistant falciparum, menispermum-dauricum, oxoisoaporphines, plasmodium selectivity @article{RN126, title = {Synthesis and Antiplasmodial Activity of Some 1-Azabenzanthrone Derivatives}, author = { V. Castro-Castillo and C. Suarez-Rozas and A. Pabon and E.G. Perez and B.K. Cassels and S. Blair}, url = {/brokenurl#<Go to ISI>://WOS:000312267700060}, doi = {10.1016/j.bmcl.2012.10.092}, issn = {0960-894x}, year = {2013}, date = {2013-01-01}, journal = {Bioorganic & Medicinal Chemistry Letters}, volume = {23}, number = {1}, pages = {327-329}, publisher = {2012 Elsevier Ltd.}, 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.}, keywords = {alkaloids antimalarial, chloroquine-resistant falciparum, menispermum-dauricum, oxoisoaporphines, plasmodium selectivity}, pubstate = {published}, tppubtype = {article} } 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. |
2013 |
Synthesis and Antiplasmodial Activity of Some 1-Azabenzanthrone Derivatives Artículo de revista Bioorganic & Medicinal Chemistry Letters, 23 (1), pp. 327-329, 2013, ISSN: 0960-894x. |