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. 2007 Aug 1;17(15):4191-5.
doi: 10.1016/j.bmcl.2007.05.041. Epub 2007 May 18.

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

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 et al. Bioorg Med Chem Lett. .

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.

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