Allosteric inhibitors of Akt1 and Akt2: Discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity

作者：Li Yiwei^*; Liang Jun; Siu Tony; Hu Essa; Rossi Michael A; Barnett Stanley F; Defeo Jones Deborah; Jones Raymond E; Robinson Ronald G; Leander Karen; Huber Hans E; Mittal Sachin; Cosford Nicholas; Prasit Peppi

来源：Bioorganic & Medicinal Chemistry Letters, 2009, 19(3): 834-836.

DOI：10.1016/j.bmcl.2008.12.017

• Akt
• Inhibitors
• Allosteric
• Cancer
• Kinase
• In vivo activity

A series of [1,2,4]triazolo[3,4-f][1,6] naphthyridine allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been shown to have potent dual Akt1 and 2 cell potency. The representative compound 13 provided potent inhibitory activity against Akt1 and 2 in vivo in a mouse model.

• 出版日期2009-2-1