@article{PAR00004660, title = {{S}ynthesis and antiplasmodial activity of new indolone {N}-oxide derivatives}, author = {{N}epveu, {F}ran{\c{c}}oise and {K}im, {S}. and {B}oyer, {J}. and {C}hatriant, {O}. and {I}brahim, {H}. and {R}eybier, {K}. and {M}onje, {M}. {C}. and {C}hevalley, {S}{\`e}verine and {P}erio, {P}. and {L}ajoie, {B}. {H}. and {B}ouajila, {J}. and {D}eharo, {E}ric and {S}auvain, {M}ichel and {T}ahar, {R}achida and {B}asco, {L}eonardo and {P}antaleo, {A}. and {T}urini, {F}. and {A}rese, {P}. and {V}alentin, {A}. and {T}hompson, {E}. and {V}ivas, {L}. and {P}etit, {S}. and {N}allet, {J}. {P}.}, editor = {}, language = {{ENG}}, abstract = {{A} series of 66 new indolone-{N}-oxide derivatives was synthesized with three different methods. {C}ompounds were evaluated for in vitro activity against {CQ}-sensitive (3{D}7), {CQ}-resistant ({F}c{B}1), and {CQ} and pyrimethamine cross-resistant ({K}1) strains of {P}lasmodium falciparum ({P}.f.), its well as for cytotoxic concentration ({CC}50) on {MCF}7 and {KB} human tumor {C}ell lines. {C}ompound 26 (5-methoxy-indolone-{N}-oxide analogue) had the most potent antiplasmodial activity in vitro (< 3 n{M} on {F}c{B}1 and = 1.7 n{M} on 3{D}7) with a very satisfactory selectivity index ({CC}50 {MCF}7/{IC}50 {F}c{B}1: 14623; {CC}50 {KB}/{IC}50 3{D}7: 198823). {I}n in vivo experiments, compound 1 (dioxymethylene derivatives of the indolone-{N}-oxide) showed the best antiplasmodial activity against {P}lasmodium berghei, 62% inhibition of the parasitaemia at 30 mg/kg/day.}, keywords = {}, booktitle = {}, journal = {{J}ournal of {M}edicinal {C}hemistry}, volume = {53}, numero = {2}, pages = {699--714}, ISSN = {0022-2623}, year = {2010}, DOI = {10.1021/jm901300d}, URL = {https://www.documentation.ird.fr/hor/{PAR}00004660}, }