Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents |
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| Institution: | 1. Institute of Applied Mathematics and Physics, Shanghai DianJi University, Shanghai 201306, People''s Republic of China;2. National Synchrotron Radiation Laboratory, University of Science and Technology of China, Hefei 230029, People''s Republic of China;3. National Energy Technology Laboratory, United States Department of Energy, Pittsburgh, PA 15236, USA |
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| 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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| Keywords: | Indolequinones Cytotoxicity Pharmacophore model |
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