Author/Authors :
Zhicai Wu، نويسنده , , Ronald G. Robinson، نويسنده , , Sheng Fu، نويسنده , , Stanley F. Barnett، نويسنده , , Deborah Defeo-Jones، نويسنده , , Raymond E. Jones، نويسنده , , Astrid M. Kral، نويسنده , , Hans E. Huber، نويسنده , , Nancy E. Kohl، نويسنده , , George D. Hartman، نويسنده , , Mark T. Bilodeau، نويسنده ,
Abstract :
This paper describes the rapid assembly of four different classes of potent Akt inhibitors from a common intermediate. Among them, a pyridopyrimidine series displayed the best intrinsic and cell potency against Akt1 and Akt2. This series also showed a promising pharmacokinetic profile and excellent selectivity over other closely related kinases.
Keywords :
Akt inhibitor , Allosteric , Rapid assembly , cancer , kinase
