13040-21-6Relevant articles and documents
Structural optimization of diphenylpyrimidine scaffold as potent and selective epidermal growth factor receptor inhibitors against L858R/T790M resistance mutation in nonsmall cell lung cancer
Yi, Yuanyuan,Wang, Luhong,Zhao, Dan,Huang, Shanshan,Wang, Changyuan,Liu, Zhihao,Sun, Huijun,Liu, Kexin,Ma, Xiaodong,Li, Yanxia
, p. 1988 - 1997 (2018)
A new class of thiodiphenylpyrimidine analogs (Thio-DPPY) were synthesized as potent and selective EGFR T790M inhibitors to overcome gefitinib resistance in nonsmall cell lung cancer (NSCLC). This structural optimization led to the identification of two p
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.
Novel 4-substituent-N-(1-substituent-1H-pyrazol-4-yl)-5-morpholinopyrimidin-2-amine derivatives and use thereof
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Paragraph 0218; 0219; 0226-0229, (2021/02/02)
A novel 4 -substituted - N N - (1-substituted - 111H-pyra -4 - yl) -5 - morpholinopyrimidine -2 - amine derivative compound or a pharmaceutically acceptable salt thereof. A pharmaceutical composition for preventing or treating JAK3-related diseases and a method for preventing or treating JAK3-related diseases using the same as an active ingredient are provided.