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. 2013 May 1;23(9):2683-7.
doi: 10.1016/j.bmcl.2013.02.082. Epub 2013 Feb 27.

Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors

Rong Jiang  1 , Bozena Frackowiak, Youseung Shin, Xinyi Song, Weimin Chen, Li Lin, Michael D Cameron, Derek R Duckett, Theodore M Kamenecka
Affiliations

Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors

Rong Jiang et al. Bioorg Med Chem Lett. .

Abstract

Starting from pyrazole HTS hit (1), a series of 1-aryl-1H-indazoles have been synthesized as JNK3 inhibitors with moderate selectivity against JNK1. SAR studies led to the synthesis of 5r as double digital nanomolar JNK3 inhibitor with good in vivo exposure.

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