期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 16, 页码 3919-3922出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.06.044
关键词
Indolequinones; Anti-T. cruzi; Cytotoxicity; Pharmacophore model
资金
- FONDECYT-Chile [1110749]
- PROMEP-Mexico [103.5-10-5345]
- CSIC-UdelaR-Uruguay [661]
- ANII-Uruguay
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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