Abstract
A cobaltoceniumethynyl gold(i) complex with a triphenylphosphane ligand triggered efficient cytotoxic effects in cancer cells in contrast to a derivative with two cobaltocenium moieties. The complex effectively inhibited the enzyme thioredoxin reductase (TrxR) suggesting this enzyme as a possible biological target. The cellular uptake of both metal fragments of the active complex was studied by atomic absorption spectroscopy and indicated a high biological stability of the complex.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cobalt / chemistry
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Cobalt / pharmacology*
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Coordination Complexes / chemical synthesis
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Coordination Complexes / chemistry
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Coordination Complexes / pharmacology*
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Gold / chemistry
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Gold / pharmacology*
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HT29 Cells
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Humans
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Molecular Structure
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Structure-Activity Relationship
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Thioredoxin-Disulfide Reductase / antagonists & inhibitors*
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Thioredoxin-Disulfide Reductase / metabolism
Substances
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Antineoplastic Agents
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Coordination Complexes
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Enzyme Inhibitors
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Cobalt
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Gold
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Thioredoxin-Disulfide Reductase