酪氨酸激酶
脾脏
酪氨酸
布鲁顿酪氨酸激酶
受体酪氨酸激酶
化学
酪氨酸激酶抑制剂
淋巴瘤
激酶
生物化学
癌症研究
生物
药理学
癌症
信号转导
免疫学
遗传学
作者
Jiayi Shen,Xiaokai Li,Zhang Zhang,Jingfeng Luo,Huoyou Long,Zhengchao Tu,Xiao‐Ping Zhou,Ke Ding,Xiaoyun Lu
摘要
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.
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