1131041-59-2Relevant academic research and scientific papers
HETEROCYCLIC KINASE INHIBITORS AND PRODUCTS AND USES THEREOF
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Page/Page column 206, (2021/01/23)
Compounds are provided having the structure of Formula (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, tautomer, isotope, or salt thereof, wherein A, X, R3, R5, R6, R7, R8, Y
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles
Lin, Hong,Yamashita, Dennis S.,Zeng, Jin,Xie, Ren,Verma, Sharad,Luengo, Juan I.,Rhodes, Nelson,Zhang, Shuyun,Robell, Kimberly A.,Choudhry, Anthony E.,Lai, Zhihong,Kumar, Rakesh,Minthorn, Elisabeth A.,Brown, Kristin K.,Heerding, Dirk A.
scheme or table, p. 679 - 683 (2010/07/06)
A novel series of AKT inhibitors containing 2,3,5-trisubstituted pyridines with novel azaindazoles as hinge binding elements are described. Among these, the 4,7-diazaindazole compound 2c has improved drug-like properties and kinase selectivity than those of indazole 1, and displays greater than 80% inhibition of GSK3β phosphorylation in a BT474 tumor xenograft model in mice.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 9; 35-36, (2009/04/25)
Invented are novel substituted pyridine compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
