Download MendeleyStructure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
Nie, Z., Perretta, C., Erickson, P., Margosiak, S., Almassy, R., Lu, J., Averill, A., Yager, K.M., Chu, S.(2007) Bioorg Med Chem Lett 17: 4191-4195
- PubMed: 17540560
- DOI: https://doi.org/10.1016/j.bmcl.2007.05.041
- Primary Citation of Related Structures:
2PVH, 2PVJ, 2PVK, 2PVL, 2PVM, 2PVN - PubMed 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.
Organizational Affiliation:
Department of Medicinal Chemistry, Polaris Pharmaceuticals Inc., San Diego, CA 92121, USA. zhe.nie@takedasd.com
