期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 10, 页码 908-912出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.6b00209
关键词
PI3K-delta; PI3K-gamma; phosphatidylinositol-4,5-bisphosphate 3-kinase-delta; p110-delta; p110-gamma; kinase inhibitor
Dual inhibition of PI3K-delta and PI3K-gamma is an established therapeutic strategy for treatment of hematological malignancies. Reported molecules targeting PI3K-delta/gamma selectively are chemically similar and based upon isoquinolin-1(2H)-one or quinazolin-4(3H)-one scaffolds. Here we report a chemically distinct series of potent, selective PI3K-delta/gamma inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold with comparable biochemical potency and cellular effects on PI3K signaling. We envisage these molecules will provide useful leads for development of next-generation PI3K-delta/gamma targeting therapeutics.
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