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

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• 作者：Zhe Nie ; Carin Perretta ; Philip Erickson ; Stephen Margosiak ; Robert Almassy ; Jia Lu ; April Averill ; Kraig M. Yager ; Shaosong Chu
• 关键词：CK2 ; Anticancer
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 August 2007
• 卷：17
• 期：15
• 页码：4191-4195
• 文件大小：701 K

摘要

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.