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
Department of Therapeutic Discovery, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
Department of Pharmacokinetics and Drug Metabolism, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, United States.
Bioorg Med Chem Lett. 2015 Mar 1;25(5):1104-9. doi: 10.1016/j.bmcl.2015.01.001. Epub 2015 Jan 17.
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.
2,3,4-取代喹啉类化合物，如(10a)，在生化和细胞实验中被发现是PI3Kδ的有效抑制剂，对其他三种I类PI3K亚型具有良好的选择性。其中一些类似物显示出良好的药代动力学性质。
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