Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2

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 μM-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.

Graphical abstractStructure-guided modifications to a series of pyrazolo[1,5-a][1,3,5]triazine derivatives provided pM inhibitors of protein kinase CK2 with low μM cytotoxic activity in cell-based assays with prostate and colon cancer cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide