1000802-52-7Relevant articles and documents
Design, synthesis and SAR study of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors
Diao, Yanyan,Ge, Huan,Li, Honglin,Liu, Dandan,Liu, Wenjun,Xu, Fangling,Xu, Yufang,Zhao, Zhenjiang,Zhu, Lili
supporting information, (2022/02/14)
The abnormal activation of JAK2 kinase is closely related to the occurrence and progression of myeloproliferative neoplasms (MPNs). At present, there is still an obvious unmet medical need for selective JAK2 inhibitors in clinic. In this paper, a class of 2-aminopyridine derivatives as potent and selective JAK2 inhibitors was obtained by combining drug design, synthesis and structure-activity relationship studies based on the previously identified lead Crizotinib. Among them, 21b exhibited high inhibitory activity against JAK2 with an IC50 of 9 9 nmol/L, moreover, it showed 276- and 184-fold selectivity over JAK1 and JAK3, respectively. Besides, 21b had a significant antiproliferative activity against HEL cells, and also inhibited the phosphorylation of JAK2 and its down-stream signaling pathway. These results indicated that 2-aminopyridine compound 21b had the potential to be developed as a selective JAK2 inhibitor for further study.
Imidazo [1, 2 - a] pyridine derivatives and preparation method and application thereof (by machine translation)
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Paragraph 0116; 0126, (2019/07/29)
The invention discloses 3 -phenyl imidazo [1, 2 - a] pyridine derivatives represented by a formula (I) or 3 - (thiophene -2 substituted) imidazo [1, 2 - a] pyridine derivatives and a preparation method, and also discloses application. of the 3 -phenyimidazo [1, 2 - a] pyridine derivatives or 3 - (thiophene -2 substituted) imidazo [1, 2 - a] pyridine derivatives as a class of novel structural novel small molecule inhibitors, and the like. (by machine translation)
Hetaryl-[1,8]naphthyridine derivatives
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Paragraph 0306; 0307; 0308, (2013/03/26)
Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.