Allosteric inhibitors of Akt1 and Akt2: A naphthyridinone with efficacy in an A2780 tumor xenograft model

作者：Bilodeau Mark T^*; Balitza Adrienne E; Hoffman Jacob M; Manley Peter J; Barnett Stanley F; Defeo Jones Deborah; Haskell Kathleen; Jones Raymond E; Leander Karen; Robinson Ronald G; Smith Anthony M; Huber Hans E; Hartman George D

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(11): 3178-3182.

DOI：10.1016/j.bmcl.2008.04.074

• Akt
• oncology

A series of naphthyridine and naphthyridinone allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been optimized to have potent dual activity against the activated kinase as well as the activation of Akt in cells. One molecule in particular, compound 17, has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model.

• 出版日期2008-6-1