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3‐aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors
Author(s) -
Shen Jiayi,
Li Xiaokai,
Zhang Zhang,
Luo Jingfeng,
Long Huoyou,
Tu Zhengchao,
Zhou Xiaoping,
Ding Ke,
Lu Xiaoyun
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12798
Subject(s) - tyrosine kinase , spleen , tyrosine , bruton's tyrosine kinase , receptor tyrosine kinase , chemistry , tyrosine kinase inhibitor , lymphoma , kinase , biochemistry , cancer research , biology , pharmacology , cancer , signal transduction , immunology , genetics
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.