Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors

ME McDonnell, H Bian, J Wrobel, GR Smith…

文献索引：McDonnell, Mark E.; Bian, Haiyan; Wrobel, Jay; Smith, Garry R.; Liang, Shuguang; Ma, Haiching; Reitz, Allen B. Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 4 p. 1116 - 1121

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被引用次数: 8

摘要

Abstract We designed a series of anilino-indoylmaleimides based on structural elements from literature JAK3 inhibitors 3 and 4, and our lead 5. These new compounds were tested as inhibitors of JAKs 1, 2 and 3 and TYK2 for therapeutic intervention in rheumatoid arthritis (RA). Our requirements, based on current scientific rationale for optimum efficacy against RA with reduced side effects, was for potent, mixed JAK1 and 3 inhibition, and selectivity over ...