Structure-based design and synthesis of novel macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds as potent inhibitors of protein kinase CK2 and their anticancer activities

被引：87
|
作者：
Nie, Zhe [1 ]
Perretta, Carin [1 ]
Erickson, Philip [1 ]
Margosiak, Stephen [2 ]
Lu, Jia [2 ]
Averill, April [2 ]
Almassy, Robert [3 ]
Chua, Shaosong [1 ]
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 | 2008年 / 18卷 / 02期
关键词：
CK2; kinase; anticancer;
D O I：
10.1016/j.bmcl.2007.11.074
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of macrocyclic derivatives has been designed and synthesized based on the X-ray co-crystal structures of pyrazolo[1,5-a] [1,3,5]triazines with corn CK2 (cCK2) protein. Bioassays demonstrated that these macrocyclic pyrazolo[1,5-a] [1,3,5]triazine compounds are potent CK2 inhibitors with K-i around 1.0 nM and strongly inhibit cancer cell growth with IC50 as low as similar to 100 nM. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：619 / 623
页数：5
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