- 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.
Bioorganic & medicinal chemistry letters (2009-03-31)
Paul S Humphries, Jennifer A Lafontaine, Charles S Agree, David Alexander, Ping Chen, Quyen-Quyen T Do, Lilian Y Li, Elizabeth A Lunney, Ranjan J Rajapakse, Karen Siegel, Sergei L Timofeevski, Tianlun Wang, David M Wilhite
PMID19327989
摘要
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.
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