761440-22-6Relevant articles and documents
Brigatinib intermediate, salt thereof, preparation method thereof and preparation method of brigatinib
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Paragraph 0059-0062; 0067, (2021/01/29)
The invention relates to the technical field of chemical synthesis, and particularly discloses a brigatinib intermediate, salt and a preparation method thereof, and a preparation method of brigatinib.The structural formula of the brigatinib intermediate i
2,4-dibasic miazines compound
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Paragraph 0249; 0250; 0251; 0252, (2017/08/29)
The invention belongs to the field of medical chemistry, relates to a 2,4-dibasic miazines compound and specifically relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof, a drug compound thereof and an application thereof in treating EGFR or/and ALK mediated diseases.
Nitric oxide donating anilinopyrimidines: Synthesis and biological evaluation as EGFR inhibitors
Han, Chun,Huang, Zhangjian,Zheng, Chao,Wan, Ledong,Lai, Yisheng,Peng, Sixun,Ding, Ke,Ji, Hongbin,Zhang, Yihua
, p. 82 - 90 (2013/10/01)
To search for potent nitric oxide (NO) donating epidermal growth factor receptor (EGFR) inhibitors, a series of phenylsulfonylfuroxan-based anilinopyrimidines 10a-h were synthesized and biologically evaluated. Compounds 10f-h exhibited potent inhibitory activity against EGFR L858R/T790M and were as potent as WZ4002 in inhibition of H1975 cells harboring EGFR L858R/T790M. Additionally, 10h produced high levels of NO in H1975 cells but not in normal human cells, and its antiproliferative activity was diminished by hemoglobin, an NO scavenger. Furthermore, 10h inhibited EGFR activation and downstream signaling in H1975 cells. These results suggest that the strong antiproliferative activity of 10h could be attributed to the synergic effects of high levels of NO production and inhibition of EGFR and downstream signaling in the cancer cells.