On August 7, 2018, Wang, Changyuan; Li, Si; Meng, Qiang; Sun, Xiuli; Li, Hua; Shu, Xiaohong; Sun, Huijun; Liu, Kexin; Liu, Zhihao; Ma, Xiaodong published an article.Electric Literature of 16230-24-3 The title of the article was Novel amino acid-substituted diphenylpyrimidine derivatives as potent BTK inhibitors against B cell lymphoma cell lines. And the article contained the following:
A new family of diphenylpyrimidine derivatives bearing an amino acid substituent were identified as potent BTK inhibitors. Among them, compound 7b (N-[3-[[5-chloro-2-[4-[2-[2-(methoxycarbonyl)-1-pyrrolidinyl]-2-oxoethoxy]phenylamino]-4-pyrimidinyl]amino]phenyl]-2-acrylamide), which features an L-proline substituent, was identified as the strongest BTK inhibitor, with an IC50 of 8.7 nM. Compound 7b also displayed similar activity against B-cell lymphoma cell lines as ibrutinib. Moreover, 7b exhibited low cytotoxic activity against normal PBMC cells. In addition, the acridine orange/ethidium bromide (AO/EB) staining assay, Western blot anal. and flow cytometry anal. also showed its effectiveness in interfering with B-cell lymphoma cell growth. The mol. simulation performance showed that 7b forms addnl. strong hydrogen bonds with the BTK protein. All these findings provided new clues about the pyrimidine scaffold as an effective BTK inhibitor for the treatment of B-cell lymphoma. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Electric Literature of 16230-24-3
The Article related to diphenylpyrimidine derivative preparation antitumor btk inhibitor b cell lymphoma, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Electric Literature of 16230-24-3
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics