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Bioorg Med Chem Lett. 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.

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  • 1Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.


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.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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