Lebouvier N. auteur aut IRD Jullian Valérie auteur aut IRD Desvignes I. auteur aut IRD Maurel S. auteur aut IRD Parenty A. auteur aut IRD Dorin-Semblat D. auteur aut IRD Doerig C. auteur aut IRD Sauvain Michel auteur aut IRD Laurent Dominique auteur aut IRD text journalArticle eng text/pdf born digital access As part of our search for new antimalarial drugs in South Pacific marine sponges, we have looked for inhibitors of Pfnek-1, a specific protein kinase of Plasmodium falciparum. On the basis of promising activity in a preliminary screening, the ethanolic crude extract of a new species of Pseudoceratina collected in Vanuatu was selected for further investigation. A bioassay-guided fractionation led to the isolation of a derivative of homogentisic acid [methyl (2,4-dibromo-3,6-dihydroxyphenyl)acetate, 4a] which inhibited Pfnek-1 with an IC50 around 1.8 mu M. This product was moderately active in vitro against a FcB1 P. falciparum strain (IC50 = 12 mu M). From the same sponge, we isolated three known compounds [11,19-dideoxyfistularin-3 (1), 11-deoxyfistularin-3 (2) and dibromo-verongiaquinol (3)] which were inactive against Pfnek-1. Synthesis and biological evaluation of some derivatives of 4a are reported. specialized Pseudoceratina Pfnek-1 homogentisic acid derivatives Plasmodium falciparum 052 035 7 4 640-653 2009 1660-3397 https://www.documentation.ird.fr/hor/fdi:010049155 10.3390/md7040640 1660-3397 [F B010049155] https://www.documentation.ird.fr/hor/fdi:010049155 https://www.documentation.ird.fr/intranet/publi/2010/01/010049155.pdf Accès réservé (Intranet de l'IRD) IRD - Base Horizon / Pleins textes 2010-02-08 2017-08-23 fdi:010049155 fre