Author/Authors :
Zhicai Wu، نويسنده , , John C. Hartnett، نويسنده , , Lou Anne Neilson، 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 , , George D. Hartman، نويسنده , , Mark T. Bilodeau، نويسنده ,
Abstract :
This communication reports a new synthetic route of pyridopyrimidines to facilitate their structural optimization in a library fashion and describes the development of pyridopyrimidines that have excellent enzymatic and cell potency against Akt1 and Akt2. This series also shows a high level of selectivity over other closely related kinases and significantly improved caspase-3 activity with the more optimized compounds.
Keywords :
Pyridopyrimidine , cancer , Akt , kinase