Abstract
A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of 6p with the Aurora-B kinase.
Publication types
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Research Support, Non-U.S. Gov't
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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Aurora Kinase B
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Aurora Kinases
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Humans
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Inhibitory Concentration 50
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Molecular Dynamics Simulation
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Picolinic Acids / chemical synthesis*
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Picolinic Acids / pharmacology*
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Protein Binding
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Protein Conformation
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology
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Protein Serine-Threonine Kinases / antagonists & inhibitors
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Protein Serine-Threonine Kinases / chemistry
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Sulfhydryl Compounds / chemical synthesis*
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Sulfhydryl Compounds / pharmacology*
Substances
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Antineoplastic Agents
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N-methyl-picolinamide-4-thiol
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Picolinic Acids
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Protein Kinase Inhibitors
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Sulfhydryl Compounds
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AURKB protein, human
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Aurora Kinase B
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Aurora Kinases
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Protein Serine-Threonine Kinases