Twenty seven lycorine derivatives were prepared and evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum. The best antiplasmodial activities were achieved with lycorine derivatives that present free hydroxyl groups at C-1 and C-2 or esterified as acetates or isobutyrates. The double bond C-2-C-3 is also important for the activity. Concerning to the antiplasmodial activity of the secolycorines, the higher values were obtained with the replacement of the methylenedioxy moiety by hydroxyl or acetate groups and with methyl substituent attached to the nitrogen atom.
Bibliographical noteFunding Information:
This work has been partly funded by the Spanish MEC ( SAF 2006-06720 and SAF 2009-13296-C02-01 ) and by the ICIC (Instituto Canario de Investigación del Cáncer) . J.C.C. thanks Gobierno Autónomo de Canarias for a predoctoral fellowship.
- Plasmodium falciparum