76870-09-2Relevant articles and documents
Diaryl urea compound as well as preparation method and pharmaceutical application thereof
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Paragraph 0053-0054; 0057-0058, (2021/05/08)
The invention belongs to the field of medicinal chemistry, and discloses a novel diarylurea compound as shown in a formula (I), physiologically acceptable salts, solvates and crystal forms of the novel diarylurea compound, a preparation method of the comp
JAK3 inhibitors based on thieno[3,2-d]pyrimidine scaffold: design, synthesis and bioactivity evaluation for the treatment of B-cell lymphoma
Chi, Fuyun,Chen, Lixue,Wang, Changyuan,Li, Lei,Sun, Xiuli,Xu, Youjun,Ma, Tengyue,Liu, Kexin,Ma, Xiaodong,Shu, Xiaohong
, (2020/01/08)
JAK3 is predominantly expressed in hematopoietic cells and has been a promising therapeutic target for the treatment of B-cell lymphoma. In this study, a new class of thieno[3,2-d]pyrimidines harboring acrylamide pharmacophore were synthesized as potent covalent JAK3 inhibitors (IC50 50 values of 1.9 nM and 1.8 nM, respectively. Furthermore, compared with the reference agents, Spebrutinib and Ibrutinib, 9a not only demonstrated enhanced antiproliferative activity against B lymphoma cells, but also showed very weak proliferative inhibition against normal peripheral blood mononuclear cells (PBMCs) at a concentration of 20 μM. Analysis of the mechanism revealed that 9a could induce the obvious apoptosis in B lymphoma cells and prevent JAK3-STAT3 cascade as well as BTK pathway. Taken together, 9a may be served as a potential new JAK3 inhibitor for the treatment of B-cell lymphoma.
(E)-3-(Aryl(arylamino)methylene)indolin-2-one derivatives: An efficient synthetic approach and evaluation of their cancer inhibitory activity
Jiang, Hongwu,Feng, Zhiyuan,Chen, Taiping,Li, Zicheng,Huang, Wencai,Luo, Youfu,Zhao, Yinglan
, p. 44 - 49 (2018/02/28)
A series of (E)-3-(aryl(arylamino)methylene)indolin-2-one derivatives were synthesised using an efficient synthetic approach. The method involved reaction of 3-bromo-3-(bromo(aryl)methyl)indolin-2-one with substituted anilines through nucleophilic substitution and a simultaneous elimination using NaHCO3 in DMF. The anticancer activity of the products against four cell lines, HCT-116, A549, SKOV3 and MDA-MB-231, was also evaluated, and several compounds showed moderate inhibitory activity.