Bioorganic and medicinal chemistry (2019)
Update date:2022-08-30
Topics:
Chang, Xiayun
Gao, Yong
He, Xiangyi
Lu, Peng
Ren, Jing
Shi, Wei
Wang, Qinglin
Wang, Xiaojin
Xu, Hongjiang
Zhang, Xiquan
Zhang, Yinsheng
Zhao, Damin
Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are very promising targets for hematological malignancies and autoimmune diseases. In recent years, a few compounds have been approved as a marketed medicine, and several are undergoing clinical trials. By recombining the dominant backbone of known active compounds, constructing a foused library, and screening a broad panel of kinases, we found a class of compounds with dual activities of anti-BTK and anti-JAK3. Some of the compounds have shown 10-folds more active in the enzyme and cell-based assays than a known active compound. Furthermore, liver microsome stability experiments show that these compounds have better stability than ibrutinib. These explorations offered new clues to discover benzoxaborole fragment and pyrimidine scaffold as more effective BTK and JAK3 dual inhibitors.
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