@article{fdi:010053425,
  title = {{T}rypanocidal properties, structure-activity relationship and computational studies of quinoxaline 1,4-di-{N}-oxide derivatives},
  author = {{E}stevez, {Y}. and {Q}uiliano, {M}. and {B}urguete, {A}. and {C}abanillas, {B}. and {Z}imic, {M}. and {M}alaga, {E}. and {V}erastegui, {M}. and {P}erez-{S}ilanes, {S}. and {A}ldana, {I}. and {M}onge, {A}. and {C}astillo, {D}. and {D}eharo, {E}ric},
  editor = {},
  language = {{ENG}},
  abstract = {{P}yrazole and propenone quinoxaline derivatives were tested against intracellular forms of {L}eishmania peruviana and {T}rypanosoma cruzi. {B}oth series were tested for toxicity against proliferative and non-proliferative cells. {T}he pyrazole quinoxaline series was quite inactive against {T}. cruzi; however, the compound 2,6-dimethyl-3-f-quinoxaline 1,4-dioxide was found to inhibit 50% of {L}eishmania growth at 8.9 mu {M}, with no impact against proliferative kidney cells and with low toxicity against {THP}-1 cells and murine macrophages. {T}he compounds belonging to the propenone quinoxaline series were moderately active against {T} cruzi. {A}mong these compounds, two were particularly interesting, (2{E})-1-(7-fluoro-3-methyl-quinoxalin-2-yl)-3-(3,4,5-trimethoxy-phenyl)-p ropenone and (2{E})-3-(3,4,5-trimethoxy-phenyl)-1-(3,6,7-trimethyl-quinoxalin-2-yl)-pro penone. {T}he former possessed selective activity against proliferative cells (cancer and parasites) and was inactive against murine peritoneal macrophages: the latter was active against {L}eishmania and inactive against the other tested cells. {F}urthermore, in silico studies showed that both series respected {L}ipinski's rules and that they confirmed a linear correlation between trypanocidal activities and {L}og{P}. {D}ocking studies revealed that compounds of the second series could interact with the poly ({ADP}-ribose) polymerase protein of {T}rypanosoma cruzi.},
  keywords = {{Q}uinoxaline 1,4-di-{N}-oxide derivatives ; {L}eishmania peruviana ; {T}rypanosoma cruzi},
  booktitle = {},
  journal = {{E}xperimental {P}arasitology},
  volume = {127},
  numero = {4},
  pages = {745--751},
  ISSN = {0014-4894},
  year = {2011},
  DOI = {10.1016/j.exppara.2011.01.009},
  URL = {https://www.documentation.ird.fr/hor/fdi:010053425},
}