Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun N-terminal kinase inhibitors

被引：7

作者：

Song, Xinyi ^{[1
]}

He, Yuanjun ^{[1
]}

Koenig, Marcel ^{[1
]}

Shin, Youseung ^{[1
]}

Noel, Romain ^{[1
]}

Chen, Weimin ^{[1
]}

Ling, Yuan Yuan ^{[1
]}

Feurstein, Daniel ^{[1
]}

Lin, Li ^{[1
]}

Ruiz, Claudia H. ^{[1
]}

Cameron, Michael D. ^{[1
]}

Duckett, Derek R. ^{[1
]}

Kamenecka, Theodore M. ^{[1
]}

机构：

[1] Scripps Res Inst, Dept Mol Therapeut & Translat Res Inst, Jupiter, FL 33458 USA

来源：

MEDCHEMCOMM | 2012年 / 3卷 / 02期

关键词：

PROTEIN-KINASE; SIGNAL-TRANSDUCTION; ACTIVATION DOMAIN; PHOSPHORYLATION; STRESS; CARCINOMA; ATF-2; BINDS; JNK1;

D O I：

10.1039/c1md00219h

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The design and synthesis of a potent series of c-jun N-terminal kinase (JNK2) inhibitors is described. The development and optimization of the 2,4-diaminopyrimidines series was carried out from an earlier in-house kinase inhibitor program. Through the optimization of the scaffold 2, several cell potent compounds with good in vivo profiles were discovered.

引用

页码：238 / 243

页数：6

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