On January 1, 2018, Ge, Yang; Wang, Changyuan; Song, Shijie; Huang, Jiaxin; Liu, Zhihao; Li, Yongming; Meng, Qiang; Zhang, Jianbin; Yao, Jihong; Liu, Kexin; Ma, Xiaodong; Sun, Xiuli published an article.Application of 16230-24-3 The title of the article was Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. And the article contained the following:
The BTK and JAK3 receptor tyrosine kinases are two validated and therapeutically amenable targets in the treatment of B-cell lymphomas. Here the authors report the identification of several classes of pyrimidine derivatives as potent BTK and JAK3 dual inhibitors. Among these mols., approx. two thirds displayed strong inhibitory capacity at less than 10 nM concentration, and four compounds could significantly inhibit the phosphorylation of BTK and JAK3 enzymes at concentrations lower than 1 nM. Addnl., these pyrimidine derivatives also exhibited enhanced activity to block the proliferation of B-cell lymphoma cells compared with the representative BTK inhibitor ibrutinib. In particular, two structure-specific compounds I and II displayed stronger activity than reference agents in cell-based evaluation, with IC50 values lower than 10 μM. Further biol. studies, including flow cytometric anal., and a xenograft model for in vivo evaluation, also indicated their efficacy and low toxicity in the treatment of B-cell lymphoma. These findings provide a new insight for the development of novel anti-B-cell lymphoma drugs with multitarget actions. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3
The Article related to btk jak3 inhibitor antitumor neoplasm, btk, inhibitor, jak3, lymphoma, pyrimidine, Pharmacology: Structure-Activity and other aspects.Application of 16230-24-3
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