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  • Title: Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents.
    Author: Tapia RA, Salas CO, Vázquez K, Espinosa-Bustos C, Soto-Delgado J, Varela J, Birriel E, Cerecetto H, González M, Paulino M.
    Journal: Bioorg Med Chem Lett; 2014 Aug 15; 24(16):3919-22. PubMed ID: 25008454.
    Abstract:
    A new indole-4,9-dione and their phenoxy derivatives were synthesized and evaluated in vitro against the epimastigote form of Trypanosoma cruzi, Y strain. All of these novel compounds were found to be extremely potent and selective that the standard drug nifurtimox. Interestingly, phenoxyindole-4,9-dione 9d displayed excellent nanomolar inhibitory activity, IC50=20 nM, and high selectivity index, SI=625. In silico studies using MOE program were performed to generate a preliminary pharmacophore model.
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