title: Synthesis and antiplasmodial activity of lycorine derivatives.
abstract: 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.
authors.affiliation: Instituto Universitario de Bio-Orgánica 'Antonio González', Av. Astrofísico Francisco Sánchez 2, 38206 La Laguna-Tenerife, Spain.
authors.forename: Juan C
authors.initials: JC
authors.lastname: Cedrón
authors.forename: David
authors.initials: D
authors.lastname: Gutiérrez
authors.forename: Ninoska
authors.initials: N
authors.lastname: Flores
authors.forename: Angel G
authors.initials: AG
authors.lastname: Ravelo
authors.forename: Ana
authors.initials: A
authors.lastname: Estévez-Braun
mesh_terms: D047151:Amaryllidaceae Alkaloids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010617:Phenanthridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D047151:Amaryllidaceae Alkaloids; D000962:Antimalarials; D010617:Phenanthridines; C015330:lycorine