Abstract
A series of variously functionalized selenium-containing compounds were purposely synthesized and evaluated against a panel of cancer cell lines. Most of the compounds showed an interesting cytotoxicity profile with compound 5 showing a potent activity on MCF7 cells. The ethyl amino derivative 5 acts synergistically with cis-platin and inhibits the GST enzyme with a potency that well correlates with the cytotoxicity observed in MCF7 cells. A computational analysis suggests a possible binding mode on the GST enzyme. As the main outcome of the present study, the ethyl amino derivative 5 emerged as a valid lead compound for further, future developments.
Keywords:
benzisoselenazolone; breast cancer; diselenide; glutathione S-transferase.
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 Proliferation / drug effects*
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Cytotoxins / chemical synthesis
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Cytotoxins / chemistry
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Cytotoxins / pharmacology
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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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Glutathione Transferase / antagonists & inhibitors*
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Glutathione Transferase / metabolism
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HeLa Cells
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Human Umbilical Vein Endothelial Cells
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Humans
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K562 Cells
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MCF-7 Cells
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Neoplasm Proteins / antagonists & inhibitors*
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Neoplasm Proteins / metabolism
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Organoselenium Compounds* / chemical synthesis
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Organoselenium Compounds* / chemistry
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Organoselenium Compounds* / pharmacology
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Selenium Compounds* / chemical synthesis
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Selenium Compounds* / chemistry
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Selenium Compounds* / pharmacology
Substances
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Antineoplastic Agents
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Cytotoxins
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Enzyme Inhibitors
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Neoplasm Proteins
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Organoselenium Compounds
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Selenium Compounds
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Glutathione Transferase