16230-24-3Relevant articles and documents
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis
Huang, Zhenhua,Zhang, Qian,Yan, Lianzhong,Zhong, Guizhen,Zhang, Linqi,Tan, Xiaojuan,Wang, Yanli
, p. 1954 - 1957 (2016)
By applying conformational restrictions, we were able to discover highly potent 1,3-diaminopyrimidine based covalent inhibitors of BTK, such as 8a (IC50 = 3.76 nM), and providing useful information of its active conformation. We are developing these novel small molecule covalent inhibitors of BTK toward oral agents for Rheumatoid arthritis.
Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity
Teng, Yu,Li, Xinyu,Ren, Shengnan,Cheng, Yu,Xi, Kun,Shen, Hongtao,Ma, Wenzhuo,Luo, Guoshun,Xiang, Hua
, (2020)
Inhibition of PI3Kδ has been proved to be an efficacious strategy for the treatment of hematological malignancies where the PI3K/Akt signaling pathway is hyperactive. Herein, a series of quinazoline derivatives bearing acrylamide fragment were prepared using skeleton-deconstruction strategy. The preliminary bioactivity evaluation resulted in the discovery of lead compound 15c. Compound 15c exhibited excellent enzyme activity against PI3Kδ (IC50 = 27.5 nM) compared with BEZ235 as well as the significant anti-proliferation activities. With the high selectivity over other PI3K isoforms and potent effects on PI3K/Akt pathway, 15c can be identified as a promising PI3Kδ inhibitor worthy of further profiling.
Synthesis and biological activity of imidazole group-substituted arylaminopyrimidines (IAAPs) as potent BTK inhibitors against B-cell lymphoma and AML
Li, Si,Wu, Bin,Zheng, Xu,Wang, Changyuan,Zhao, Jingyuan,Sun, Huijun,Sun, Xiuli,Tang, Zeyao,Yuan, Hong,Chen, Lixue,Ma, Xiaodong
, (2020/12/07)
Bruton's tyrosine kinase (BTK) is a member of the Tec kinase family and plays a key role in the modulation of the B-cell receptor (BCR)-mediated signaling pathway. Inhibition of BTK has been proven to be an effective therapeutic approach for various hemat
S-triazine compounds as well as preparation method and application thereof
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Paragraph 0069; 0072, (2020/05/05)
The invention discloses s-triazine compounds and pharmaceutically acceptable salts thereof; experiments prove that the compounds can be used for treating or preventing diseases related to protein kinase activity, such as leukemia and lymphoma, by inhibiti