1131041-72-9Relevant articles and documents
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines
Lin, Hong,Yamashita, Dennis S.,Xie, Ren,Zeng, Jin,Wang, Wenyong,Leber, Jack,Safonov, Igor G.,Verma, Sharad,Li, Mei,LaFrance, Louis,Venslavsky, Joseph,Takata, Dennis,Luengo, Juan I.,Kahana, Jason A.,Zhang, Shuyun,Robell, Kimberly A.,Levy, Dana,Kumar, Rakesh,Choudhry, Anthony E.,Schaber, Michael,Lai, Zhihong,Brown, Barry S.,Donovan, Brian T.,Minthorn, Elisabeth A.,Brown, Kristin K.,Heerding, Dirk A.
scheme or table, p. 684 - 688 (2010/06/14)
The synthesis and evaluation of tetrasubstituted aminopyridines, bearing novel azaindazole hinge binders, as potent AKT inhibitors are described. Compound 14c was identified as a potent AKT inhibitor that demonstrated reduced CYP450 inhibition and an improved developability profile compared to those of previously described trisubstituted pyridines. It also displayed dose-dependent inhibition of both phosphorylation of GSK3β and tumor growth in a BT474 tumor xenograft model in mice.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 8; 33-34, (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.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 9; 37-38, (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.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 11; 42, (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.