Abstract
In the process of optimization, we developed a novel core skeleton of thieno[3,4-b]pyrazine via GK-13. The derivatives synthesized were shown to inhibit TGase 2 activity in cancer cells. Some of the hit compounds such as the arylethynyl group-coupled thieno[3,4-b]pyrazine derivatives were shown to exhibit promising activity for use as potential therapeutic small-molecules in renal cancer by inhibiting TGase 2 activity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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GTP-Binding Proteins / antagonists & inhibitors*
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Humans
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Magnetic Resonance Spectroscopy
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Molecular Docking Simulation
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Protein Glutamine gamma Glutamyltransferase 2
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Pyrazines / chemical synthesis*
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Pyrazines / chemistry
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Pyrazines / pharmacology
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Transglutaminases / antagonists & inhibitors*
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Pyrazines
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Protein Glutamine gamma Glutamyltransferase 2
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Transglutaminases
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GTP-Binding Proteins