138240-34-3Relevant articles and documents
Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors
Zhang, Yun,Xia, Anjie,Zhang, Shiyu,Lin, Guifeng,Liu, Jingming,Chen, Pei,Mu, Bo,Jiao, Yan,Xu, Wenwen,Chen, Mingxin,Li, Linli
, (2021)
Inhibition of cdc2-like kinase1 (CLK1) could efficiently induce autophagy and it has been thought as a potential target for treatment of autophagy-related diseases. Herein we report the discovery of a series of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors. Among them, compound 9e is the most potent one, which exhibits an IC50 value of 4 nM against CLK1 kinase. In vitro, this compound reduces the phosphorylation level of the typical downstream substrates of CLK1 and affects their subcellular redistribution. Further study indicates that 9e is efficient to induce autophagy. Overall, this study provides a promising lead compound for drug discovery targeting CLK1 kinase.
Preparation and application of imidazo aromatic ring compounds
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Paragraph 0151-0156, (2020/05/02)
The invention provides preparation and application of imidazo aromatic ring compounds, and particularly provides compounds as shown in the following formula I. The definition of each group is as shownin the specification. The compounds have TRK kinase inh
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis
Kim, Okseon,Jeong, Yujeong,Lee, Hyunseung,Hong, Sun-Sun,Hong, Sungwoo
experimental part, p. 2455 - 2466 (2011/06/20)
Phosphatidylinositol 3-kinase α (PI3Kα) is an important regulator of intracellular signaling pathways, controlling remarkably diverse arrays of physiological processes. Because the PI3K pathway is frequently up-regulated in human cancers, the inhibition of PI3Kα can be a promising approach to cancer therapy. In this study, we have designed and synthesized a new series of imidazo[1,2-a]pyridine derivatives as PI3Kα inhibitors through the fragment-growing strategy. By varying groups at the 3- and 6-positions of imidazo[1,2-a]pyridines, we studied the structure-activity relationships (SAR) profiles and identified a series of potent PI3Kα inhibitors. Representative derivatives showed good activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.