On July 28, 2017, Liu, He; Qu, Menghua; Xu, Lina; Han, Xu; Wang, Changyuan; Shu, Xiaohong; Yao, Jihong; Liu, Kexin; Peng, Jinyong; Li, Yanxia; Ma, Xiaodong published an article.Product Details of 16230-24-3 The title of the article was Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton’s tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. And the article contained the following:
A new series of diphenylpyrimidine derivatives (SFA-DPPYs) were synthesized by introducing a functional sulfonamide into the C-2 aniline moiety of pyrimidine template, and then were biol. evaluated as potent Bruton’s tyrosine kinase (BTK) inhibitors. Among these mols., inhibitors 10c, 10i, 10j and 10k (I – IV, resp.) displayed high potency against the BTK enzyme, with IC50 values of 1.18 nM, 0.92 nM, 0.42 nM and 1.05 nM, resp. In particular, compound 10c could remarkably inhibit the proliferation of the B lymphoma cell lines at concentrations of 6.49 μM (Ramos cells) and 13.2 μM (Raji cells), and was stronger than the novel agent spebrutinib. In addition, the inhibitory potency toward the normal PBMC cells showed that inhibitor 10c possesses low cell cytotoxicity. All these explorations indicated that mol. 10c could serve as a valuable inhibitor for B-cell lymphoblastic leukemia treatment. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Product Details of 16230-24-3
The Article related to sulfonamide phenylpyrimidine bruton tyrosine kinase inhibitor lymphoblastic leukemia, b cell lymphoblastic leukemia sulfonamide phenylpyrimidine, btk, inhibitor, leukemia, pyrimidine, sulfonamide and other aspects.Product Details of 16230-24-3
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics