Synthesis and biological evaluation of furo[2,3-d]pyrimidines as Akt1 kinase inhibitors

被引：0

作者：

Kim, Se Young ^{[1
]}

Kim, Dong Jin ^{[1
]}

Yang, Beom Seok ^{[1
]}

Yoo, Kyung Ho ^{[1
]}

机构：

[1] Korea Inst Sci & Technol, Life Sci Res Div, Seoul 130650, South Korea

来源：

BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2007年 / 28卷 / 07期

关键词：

Akt1; kinase; inhibitory activity; furo[2,3-d]pyrimidines;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Based on the hit compound 4 derived from focused library, a series of furo[2,3-d]pyrimidines were designed, synthesized and evaluated for the inhibitory activity against Akt1 kinase. And their structure-activity relationships were investigated. Of these compounds, 3a having 2-thienyl and methyl groups at R-1 and R-2 showed the most potent activity with an IC50 value of 24 mu M. Introduction of the thienyl groups at C-5 and C-6 positions significantly improved potency compared to furyl and phenyl groups.

引用

页码：1114 / 1118

页数：5

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