Article

Projet
 
Yung-Sing WONG, Marie-Ange LESPINASSE,   
Titre
Uncovering new structural insights for antimalarial activity from cost-effective aculeatin-like derivatives  
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Auteurs
Winkler, Matthias Maynadier, Marjorie Wein, Sharon Lespinasse, Marie-Ange Boumis, Giovanna Miele, Adriana E. Vial, Henri Wong, Yung-Sing
Edition
Org. Biol. Chem. 2015, 13, 2064-2077
Année
2015
Résumé
A series of new aculeatin-like analogs were synthesized in two steps by combining two sets of building blocks. Many compds. showed inhibitory activities in vitro against Plasmodium falciparum and have helped to gain more insight into structure-activity relationships around the spirocyclohexadienone pharmacophoric scaffold. Plasmodium falciparum thioredoxin reductase (PfTrxR) has been investigated as a putative cellular target. Moreover, a new aculeatin-like scaffold without Michael acceptor properties, efficient at 0.86 μM against P. falciparum 3D7, was identified and raises the prospect of developing a new antimalarial agent