864775-61-1Relevant academic research and scientific papers
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 55; 147, (2010/02/14)
Invented are novel pyridine compounds, the use of such compounds as inhibitors of PKB/AKT kinase activity and in the treatment of cancer and arthritis.
