Synthesis and SAR study of potent and selective PI3Kδ inhibitors
2,3,4-Substituted quinolines such as (10a) were found to be potent inhibitors of PI3Kδ in both biochemical and cellular assays with good selectivity over three other class I PI3K isoforms. Some of those analogs showed favorable pharmacokinetic properties.
Bui, Minna,Hao, Xiaolin,Shin, Youngsook,Cardozo, Mario,He, Xiao,Henne, Kirk,Suchomel, Julia,McCarter, John,McGee, Lawrence R.,San Miguel, Tisha,Medina, Julio C.,Mohn, Deanna,Tran, Thuy,Wannberg, Sharon,Wong, Jamie,Wong, Simon,Zalameda, Leeanne,Metz, Daniela,Cushing, Timothy D.