Antiplasmodial activity of naphthoquinones related to lapachol and beta-lapachone.
The in vitro antiplasmodial activity of 26 naphthoquinone derivatives related to the natural lapachol (1) and beta-lapachone (2) was tested. Ten of these derivatives are reported for the first time. The evaluation was performed on cultures of F32 strain of Plasmodium falciparum, and some derivatives displayed attractive in vitro activities (IC50 < 10 microM). Based on these results, some structure-activity relationships have been determined.
Pérez-Sacau
Elisa
E
Instituto Universitario de Bio-Orgánica Antonio González. Avda. Astrofísico Francisco Sánchez No2, E-38206 La Laguna, Tenerife.
Estévez-Braun
Ana
A
Ravelo
Angel G
AG
Gutiérrez Yapu
David
D
Giménez Turba
Alberto
A
D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D009285:Naphthoquinones / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects*
D000962:Antimalarials; D009285:Naphthoquinones; C014638:beta-lapachone; C008252:lapachol