Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2
Z. Nie, C. Perretta, P. Ericksin, S. Margosiak, R. Almassy, J. Lu, A. Averill, K.M. Yager and S. ChuBioorganic & Medicinal Chemistry Letters (2007), Vol. 17 pages 4191-4195
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 prostrate and colon cancer cell lines.