@article{fdi:010064628,
  title = {{D}iscovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of {P}lasmodium},
  author = {{C}ohen, {A}. and {S}uzanne, {P}. and {L}ancelot, {J}. {C}. and {V}erhaeghe, {P}. and {L}esnard, {A}. and {B}asmaciyan, {L}. and {H}utter, {S}. and {L}aget, {M}. and {D}umetre, {A}. and {P}aloque, {L}. and {D}eharo, {E}ric and {C}rozet, {M}. {D}. and {R}athelot, {P}. and {D}allemagne, {P}. and {L}orthiois, {A}. and {S}ibley, {C}. {H}. and {V}anelle, {P}. and {V}alentin, {A}. and {M}azier, {D}. and {R}ault, {S}. and {A}zas, {N}.},
  editor = {},
  language = {{ENG}},
  abstract = {{A} preliminary in vitro screening of compounds belonging to various chemical families from our library revealed the thieno[3,2-d]pyrimidin-4(3{H})-one scaffold displayed a promising profile against {P}lasmodium falciparum. {T}hen, 120 new derivatives were synthesized and evaluated in vitro; compared to drug references, 40 showed good activity toward chloroquine sensitive ({IC}50 35-344 n{M}) and resistant ({IC}50 45-800 n{M}) {P}. falciparum strains. {T}hey were neither cytotoxic ({CC}50 15-50 mu {M}) toward {H}ep{G}2 and {CHO} cells, nor mutagenic. {S}tructure activity relationships were defined. {T}he lead-compound also appeared active against the {P}lasmodium liver stages ({P}lasmodium yoelii {IC}50 = 35 n{M}) and a preliminary in vivo evaluation indicated the in vitro activity was preserved (45% reduction in parasitemia compared to untreated infected mice). {A} mechanistic study demonstrated these molecules do not involve any of the pathways described for commercial drugs and exert a specific activity on the ring and trophozoite stages. 2015 {E}lsevier {M}asson {SAS}. {A}ll rights reserved.},
  keywords = {{T}hieno[3,2-dlpyrimidin-4(3{H})-one ; {P}harmacomodulation ; {I}n vitro ; antiplasmodial profile ; {G}enotoxicity ; {A}ctivity against {P}lasmodium liver stages ; {A}ntiplasmodial mechanism of action},
  booktitle = {},
  journal = {{E}uropean {J}ournal of {M}edicinal {C}hemistry},
  volume = {95},
  numero = {},
  pages = {16--28},
  ISSN = {0223-5234},
  year = {2015},
  DOI = {10.1016/j.ejmech.2015.03.011},
  URL = {https://www.documentation.ird.fr/hor/fdi:010064628},
}