858117-40-5Relevant academic research and scientific papers
Nitrogen-Containing Heteroaryl Derivatives and Their Use as GSK3β Inhibitors
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Paragraph 0375; 0376; 0379, (2017/08/15)
Provided are a novel compound represented by chemical formula 1 and having GSK3β inhibitory activities, or a pharmaceutically allowable salt thereof. The compound represented by chemical formula 1 can be used for preventing or treating diseases associated with GSK3β such as proliferative disorders, neurodegenerative or neurogenic diseases, inflammatory autoimmune disorders, cardiovascular diseases, endocrinopathy and diseases by virus infection.COPYRIGHT KIPO 2017
Identification of lead small molecule inhibitors of glycogen synthase kinase-3 beta using a fragment-linking strategy
Kim, Jinhee,Moon, Yonghoon,Hong, Sungwoo
, p. 5669 - 5673 (2016/11/28)
Glycogen synthase kinase-3 beta (GSK3β) kinase serves as a promising therapeutic target for the treatment of various human diseases, such as diabetes, obesity, and Alzheimer's disease. In this study, we report lead GSK3β inhibitors identified using a fragment-linking strategy. Through the systematic exploration, a six-atom chain unit bearing the rigid double bond was found to be a suitable linker connecting two fragments, which enables favorable contacts with backbone groups of residues in the pockets. As a consequence, potent GSK3β inhibitor 9i was found with IC50values of 19 nM. The binding mode analysis indicates that the activities of the inhibitors appear to be achieved by the establishment of multiple hydrogen bonds and hydrophobic interactions in the ATP-binding site of GSK3β. The good biochemical potencies and structural uniqueness of the inhibitors support consideration in the further study to optimize the biological activity.
Pyrrolo-pyridine kinase modulators
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Page/Page column 96, (2010/02/15)
The present invention provides novel pyrrolo-pyridine kinase modulators and methods of using the novel pyrrolo-pyridine kinase modulators to treat diseases mediated by kinase activity.
