@article{fdi:010049155, title = {{A}ntiplasmodial activities of homogentisic acid derivative protein kinase inhibitors isolated from a {V}anuatu marine sponge {P}seudoceratina sp}, author = {{L}ebouvier, {N}. and {J}ullian, {V}al{\'e}rie and {D}esvignes, {I}. and {M}aurel, {S}. and {P}arenty, {A}. and {D}orin-{S}emblat, {D}. and {D}oerig, {C}. and {S}auvain, {M}ichel and {L}aurent, {D}ominique}, editor = {}, language = {{ENG}}, abstract = {{A}s part of our search for new antimalarial drugs in {S}outh {P}acific marine sponges, we have looked for inhibitors of {P}fnek-1, a specific protein kinase of {P}lasmodium falciparum. {O}n the basis of promising activity in a preliminary screening, the ethanolic crude extract of a new species of {P}seudoceratina collected in {V}anuatu 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 {P}fnek-1 with an {IC}50 around 1.8 mu {M}. {T}his product was moderately active in vitro against a {F}c{B}1 {P}. falciparum strain ({IC}50 = 12 mu {M}). {F}rom 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 {P}fnek-1. {S}ynthesis and biological evaluation of some derivatives of 4a are reported.}, keywords = {{P}seudoceratina ; {P}fnek-1 ; homogentisic acid derivatives ; {P}lasmodium ; falciparum}, booktitle = {}, journal = {{M}arine {D}rugs}, volume = {7}, numero = {4}, pages = {640--653}, ISSN = {1660-3397}, year = {2009}, DOI = {10.3390/md7040640}, URL = {https://www.documentation.ird.fr/hor/fdi:010049155}, }