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

被引：95

作者：

Nie, Zhe ^{[1
]}

Perretta, Carin

Erickson, Philip

Margosiak, Stephen

Almassy, Robert

Lu, Jia

Averill, April

Yager, Kraig M.

Chu, Shaosong

机构：

[1] Polaris Pharmaceut Inc, Dept Med Chem, San Diego, CA 92121 USA

[2] Polaris Pharmaceut Inc, Dept Prot Chem, San Diego, CA 92121 USA

[3] Polaris Pharmaceut Inc, Dept Biol Struct, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 15期

关键词：

CK2; anticancer;

D O I：

10.1016/j.bmcl.2007.05.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 mu M-level cytotoxic activity in cell-based assays with prostate and colon cancer cell lines. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4191 / 4195

页数：5

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