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Aminopurine based JNK inhibitors for the prevention of ischemia reperfusion injury

作者	Krenitsky, VP; Delgado, M; Nadolny, L; Sahasrabudhe, K; Ayala, L; Clareen, SS; Hilgraf, R; Albers, R; Kois, A; Hughes, K; Wright, J; Nowakowski, J; Sudbeck, E; Ghosh, S; Bahmanyar, S; Chamberlain, P; Muir, J; Cathers, BE; Giegel, D; Xu, L; Celeridad, M; Moghaddam, M; Khatsenko, O; Omholt, P; Katz, J; Pai, S; Fan, R; Tang, Y; Shirley, MA; Benish, B; Blease, K; Raymon, H; Bhagwat, S; Henderson, I; Cole, AG; Bennett, B; Satoh, Y

选自	期刊 Bioorganic & Medicinal Chemistry Letters; 卷期 2012年22-3; 页码 1427-1432

关联知识点

[摘要]：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. (C) 2011 Elsevier Ltd. All rights reserved.
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