Abstract
Thioredoxin (Trx) expression is increased in several human primary cancers and the Trx/Trx reductase (TrxR) system therefore provides an attractive target for cancer drug development. Novel organotellurium antioxidants, especially a primitive analog of vitamin E (compound 1d) and compounds 7, 9 and 10--all carrying highly functionalized 4-(dialkylamino)phenyltelluro groups to secure high antioxidative capacity--were found to inhibit TrxR with IC50 values in the low micromolar range. Whereas antioxidant 1d also inhibited the growth of MCF-7 human breast cancer cells in culture at a similar level (IC50 = 1.8 microM), the other TrxR inhibitors were inactive in concentrations below about 10 M.
Copyright 2003 Lippincott Williams & Wilkins
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Antioxidants / chemical synthesis
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Antioxidants / pharmacology*
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Breast Neoplasms / enzymology
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Breast Neoplasms / pathology*
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Cell Division / drug effects
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Cell Survival / drug effects
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Humans
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Organometallic Compounds / chemical synthesis
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Organometallic Compounds / pharmacology*
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Oxidation-Reduction
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Tellurium / chemistry
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Tellurium / pharmacology*
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Thioredoxin-Disulfide Reductase / antagonists & inhibitors*
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Thioredoxins / pharmacology
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Tumor Cells, Cultured
Substances
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Antioxidants
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Enzyme Inhibitors
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Organometallic Compounds
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Thioredoxins
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Thioredoxin-Disulfide Reductase
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Tellurium