On January 27, 2017, Zhao, Dan; Huang, Shanshan; Qu, Menghua; Wang, Changyuan; Liu, Zhihao; Li, Zhen; Peng, Jinyong; Liu, Kexin; Li, Yanxia; Ma, Xiaodong; Shu, Xiaohong published an article.Category: amides-buliding-blocks The title of the article was Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines. And the article contained the following:
A new series of diphenylpyrimidine derivatives (DPPYs) bearing various aniline side chains at the C-2 position of pyrimidine core were synthesized as potent BTK inhibitors. Most of these inhibitors displayed improved activity against B leukemia cell lines compared with lead compound spebrutinib. Subsequent studies showed that the peculiar inhibitor I, with IC50 values of 10.5 μM against Ramos cells and 19.1 μM against Raji cells, also displayed slightly higher inhibitory ability than the novel agent ibrutinib. Moreover, compound I is not sensitive to normal cells PBMC, indicating low cell cytotoxicity. In addition, flow cytometry anal. indicated that I significantly induced the apoptosis of Ramos cells, and arrested the cell cycle at the G0/G1 phase. These explorations provided new clues to discover pyrimidine scaffold as more effective BTK inhibitors. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Category: amides-buliding-blocks
The Article related to diphenylpyrimidine preparation bruton tyrosine kinase inhibitory activity, btk, inhibitor, leukemia, pyrimidine, synthesis, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: amides-buliding-blocks
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