@article{fdi:010073135,
  title = {{S}tructure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives : synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery},
  author = {{Q}uiliano, {M}. and {P}abon, {A}. and {M}oles, {E}. and {B}onilla-{R}amirez, {L}. and {F}abing, {I}. and {F}ong, {K}. {Y}. and {N}ieto-{A}co, {D}. {A}. and {W}right, {D}. {W}. and {P}izarro, {J}. {C}. and {V}ettorazzi, {A}. and de {C}erain, {A}. {L}. and {D}eharo, {E}ric and {F}ernandez-{B}usquets, {X}. and {G}aravito, {G}. and {A}ldana, {I}. and {G}aliano, {S}.},
  editor = {},
  language = {{ENG}},
  abstract = {{D}esign, synthesis, structure-activity relationship, cytotoxicity studies, in silico drug-likeness, genotoxicity screening, and in vivo studies of new 1-aryl-3-substituted propanol derivatives led to the identification of nine compounds with promising in vitro (55, 56, 61, 64, 66, and 70-73) and in vivo (66 and 72) antimalarial profiles against {P}lasmodium falciparum and {P}lasmodium berghei. {C}ompounds 55, 56, 61, 64, 66 and 70-73 exhibited potent antiplasmodial activity against chloroquine-resistant strain {FCR}-3 ({IC}(50)s <0.28 mu {M}), and compounds 55, 56, 64, 70, 71, and 72 showed potent biological activity in chloroquine-sensitive and multidrug-resistant strains ({IC}(50)s < 0.7 mu {M} for 3{D}7, {D}6, {FCR}-3 and {C}235). {A}ll of these compounds share appropriate drug-likeness profiles and adequate selectivity indexes (77 < {SI} < 184) as well as lack genotoxicity. {I}n vivo efficacy tests in a mouse model showed compounds 66 and 72 to be promising candidates as they exhibited significant parasitemia reductions of 96.4% and 80.4%, respectively. {A}dditional studies such as liver stage and sporogony inhibition, target exploration of heat shock protein 90 of {P}. falciparum, targeted delivery by immunoliposomes, and enantiomer characterization were performed and strongly reinforce the hypothesis of 1-aryl-3-substituted propanol derivatives as promising antimalarial compounds.},
  keywords = {{A}ntiplasmodial ; {A}ntimalarial ; {A}rylamino alcohol ; {M}ulti-stage activity ; {H}sp90 ; {E}nantiomer separation},
  booktitle = {},
  journal = {{E}uropean {J}ournal of {M}edicinal {C}hemistry},
  volume = {152},
  numero = {},
  pages = {489--514},
  ISSN = {0223-5234},
  year = {2018},
  DOI = {10.1016/j.ejmech.2018.04.038},
  URL = {https://www.documentation.ird.fr/hor/fdi:010073135},
}