Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 16, Pages 3919-3922Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.06.044
Keywords
Indolequinones; Anti-T. cruzi; Cytotoxicity; Pharmacophore model
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Funding
- FONDECYT-Chile [1110749]
- PROMEP-Mexico [103.5-10-5345]
- CSIC-UdelaR-Uruguay [661]
- ANII-Uruguay
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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. (C) 2014 Elsevier Ltd. All rights reserved.
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