Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361503 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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.
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Related Topics
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Organic Chemistry
Authors
Véronique Plantevin Krenitsky, Mercedes Delgado, Lisa Nadolny, Kiran Sahasrabudhe, Leticia Ayala, Steven S. Clareen, Robert Hilgraf, Ronald Albers, Adam Kois, Kevin Hughes, Jonathan Wright, Jacek Nowakowski, Elise Sudbeck, Sutapa Ghosh, Sogole Bahmanyar,