Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors
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DOI：
10.1016/j.bmcl.2009.03.023
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发表时间：
2009-04-15
影响因子：
2.7
通讯作者：
Wilhite, David M.
中科院分区：
文献类型：
--
作者：
Humphries, Paul S.;Lafontaine, Jennifer A.;Wilhite, David M.
介绍了一系列新型的4-取代-2-氨基嘧啶类化合物作为c-jun氨基末端酶抑制剂的研究进展。讨论了JNK1的合成、对JNK1的体外抑制值以及对c-Jun细胞的体外抑制值。微粒体清除的优化导致了9c的鉴定，其激酶选择性已被报道。(C)2009爱思唯尔有限公司。保留所有权利。
The development of a series of novel 4-substituted-2-aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, and the in vitro inhibitory value for a c-Jun cellular assay are discussed. Optimization of microsomal clearance led to the identification of 9c, whose kinase selectivity is reported. (C) 2009 Elsevier Ltd. All rights reserved.