Anilino-monoindolylmaleimides as potent and selective JAK3 inhibitors

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

Index: 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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Citation Number: 8

Abstract

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 ...

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