864775-63-3Relevant 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.
, p. 679 - 683 (2010)
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
-
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.
