On January 15, 2020, Ren, Jing; Shi, Wei; Zhao, Damin; Wang, Qinglin; Chang, Xiayun; He, Xiangyi; Wang, Xiaojin; Gao, Yong; Lu, Peng; Zhang, Xiquan; Xu, Hongjiang; Zhang, Yinsheng published an article.Category: amides-buliding-blocks The title of the article was Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. And the article contained the following:
Bruton’s tyrosine kinase (BTK) and Janus kinase 3 (JAK3) are very promising targets for hematol. malignancies and autoimmune diseases. In recent years, a few compounds have been approved as a marketed medicine, and several are undergoing clin. trials. By recombining the dominant backbone of known active compounds, constructing a focused 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. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks
The Article related to boron diphenyl pyrimidine derivative preparation btk jak3 inhibitor cancer, autoimmune disease boron diphenyl pyrimidine derivative preparation, autoimmune diseases, btk, benzoxaborole, dual inhibitor, hematological, jak3, pyrimidine and other aspects.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics