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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. vplantev@celgene.com

Abstract

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.

PMID:
22226655
[PubMed - indexed for MEDLINE]

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