Abstract
The structure-based design, synthesis, and anticancer activity of novel inhibitors of protein kinase CK2 are described. Using pyrazolo[1,5-a][1,3,5]triazine as the core scaffold, a structure-guided series of modifications provided pM inhibitors with microM-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.
MeSH terms
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Binding Sites
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Casein Kinase II / antagonists & inhibitors*
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Casein Kinase II / metabolism
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Cell Line, Tumor
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Crystallography, X-Ray
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Drug Design
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Humans
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Models, Molecular
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Molecular Structure
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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*
Substances
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Protein Kinase Inhibitors
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Casein Kinase II