128883-83-0Relevant articles and documents
Design and Synthesis of a Series of Novel Macrocycle Janus Kinase 2 Inhibitors
Wang, Yanling,Ge, Huan,Wang, Disha,He, Huan,Li, Lu,Diao, Yanyan,Shen, Zihao,Zhu, Lili,Li, Shiliang,Zhao, Zhenjiang,Li, Honglin
, p. 1259 - 1263 (2019)
Macrocycle has attracted the attention of many researchers in the field of medicinal chemistry due to its unique advantages and good prospects, but the difficulties in drug design and synthesis of macrocycle limit its applications. In this study, a series of macrocyclic derivatives designed from anaplastic lymphoma kinase (ALK) inhibitor lorlatinib were synthesized as Janus kinase 2 (JAK2) selective inhibitors. Among them, 17f had the best inhibitory activity (IC50 = 0.177 μmol·L–1) and selectivity for JAK2 over JAK1 and JAK3, which indicated that design of the macrocyclic derivatives might be a feasible strategy for the discovery of novel selective JAK2 inhibitors.
MACROCYCLIC COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Paragraph 00316; 00318, (2015/04/22)
The compounds and salts of the present invention inhibit kinases, especially the anaplastic lymphoma kinase (ALK) and the HGF receptor tyrosine kinase (RTK) c-Met, and are useful for treating or ameliorating abnormal cell proliferative disorders, such as
