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Bioorg Med Chem Lett. 2012 Feb 1;22(3):1427-32. doi: 10.1016/j.bmcl.2011.12.028. Epub 2011 Dec 11.

Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury.

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  • 1Celgene Corporation, 4550 Towne Centre Court, San Diego, CA 92121, USA.


In this Letter we describe the optimization of an aminopurine lead (1) with modest potency and poor overall kinase selectivity which led to the identification of a series of potent, selective JNK inhibitors. Improvement in kinase selectivity was enabled by introduction of an aliphatic side chain at the C-2 position. CC-359 (2) was selected as a potential clinical candidate for diseases manifested by ischemia reperfusion injury.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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