Bioorganic & Medicinal Chemistry Letters 2007-08-01

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

Zhe Nie, Carin Perretta, Philip Erickson, Stephen Margosiak, Robert Almassy, Jia Lu, April Averill, Kraig M Yager, Shaosong Chu

Index: Bioorg. Med. Chem. Lett. 17(15) , 4191-5, (2007)

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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.