1403669-14-6Relevant articles and documents
Discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2-one- containing Phosphoinositide 3-kinase (PI3K) p110β isoform inhibitors through structure-based fragment optimisation
Giordanetto, Fabrizio,W?llberg, Andreas,Cassel, Johan,Ghosal, Saswati,Kossenjans, Michael,Yuan, Zhong-Qing,Wang, Xiaoping,Liang, Lifeng
, p. 6665 - 6670 (2013/01/14)
The discovery of 4-morpholino-pyrimidin-6-one and 4-morpholino-pyrimidin-2- one-containing inhibitors of Phosphoinositide 3-kinases (PI3K) p110β isoform is reported. Structure-based optimisation of the original fragment hit resulted in lead compounds with improvements in ligand efficiency, lipophilicity efficiency, p110β potency and selectivity over p110α.