Structure-activity relationships of pyrazine-based CK2 inhibitors: Synthesis and evaluation of 2,6-disubstituted pyrazines and 4,6-disubstituted pyrimidines

被引：26
|
作者：
Suzuki, Yarnato [1 ]
Cluzeau, Jerome [1 ]
Hara, Takafumi [1 ]
Hirasawa, Akira [1 ]
Tsujimoto, Gozoh [1 ]
Oishi, Shinya [1 ]
Ohno, Hiroaki [1 ]
Fujii, Nobutaka [1 ]
机构：
[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan
来源：
ARCHIV DER PHARMAZIE | 2008年 / 341卷 / 09期
关键词：
CK2; glomerulonephritis; kinase inhibitor; pyrazine derivatives; SAR study;
D O I：
10.1002/ardp.200700269
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structually related to the known CK2 inhibitors, 2,6-disubstituted pyrazine and 4,6-disubstituted pyrimidine derivatives were synthesized and their inhibitory activities toward CK2 alpha and CK2 alpha' were evaluated. Structure-activity relationship study has revealed that several pyrazine derivatives bearing a (pyrrol-3-yl)acetic acid and a monosubstituted aniline possess potent inhibitory activities.
引用
收藏
页码：554 / 561
页数：8
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