3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors

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• 作者：Jiayi Shen ; Xiaokai Li ; Zhang Zhang ; Jingfeng Luo ; Huoyou Long ; Zhengchao Tu ; Xiaoping Zhou ; Ke Ding and Xiaoyun Lu
• 刊名：Chemical Biology & Drug Design
• 出版年：2016
• 出版时间：November 2016
• 年：2016
• 卷：88
• 期：5
• 页码：690-698
• 全文大小：1209K
• ISSN：1747-0285

文摘

Spleen tyrosine kinase is a new promising target for drug discovery to treat human cancer and inflammatory disorders. A series of pyrazolopyrazine-3-amine and pyrazolopyrimidine-3-amine derivatives was designed and synthesized as new spleen tyrosine kinase inhibitors. The efforts yielded compound 6h with promising spleen tyrosine kinase inhibition in both enzymatic and B-lymphoma cell proliferation assays. Additionally, compound 6h dose dependently inhibited the activation of spleen tyrosine kinase signal in human B-cell lymphoma cells. Compound 6h might serve as a lead for further development of new spleen tyrosine kinase inhibitors.