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- Title
3-aminopyrazolopyrazine derivatives as spleen tyrosine kinase inhibitors.
- Authors
Shen, Jiayi; Li, Xiaokai; Zhang, Zhang; Luo, Jingfeng; Long, Huoyou; Tu, Zhengchao; Zhou, Xiaoping; Ding, Ke; Lu, Xiaoyun
- Abstract
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.
- Subjects
PROTEIN-tyrosine kinases; LYMPHOMAS; CELL proliferation; SPLEEN; LYMPHOCYTES
- Publication
Chemical Biology & Drug Design, 2016, Vol 88, Issue 5, p690
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12798