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Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-delta/gamma Inhibitors
- Authors
- Ferguson, Fleur M.; Ni, Jing; Zhang, Tinghu; Tesar, Bethany; Sim, Taebo; Kim, Nam Doo; Deng, Xianming; Brown, Jennifer R.; Zhao, Jean J.; Gray, Nathanael S.
- Issue Date
- 10월-2016
- Publisher
- AMER CHEMICAL SOC
- Keywords
- PI3K-delta; PI3K-gamma; phosphatidylinositol-4,5-bisphosphate 3-kinase-delta; p110-delta; p110-gamma; kinase inhibitor
- Citation
- ACS MEDICINAL CHEMISTRY LETTERS, v.7, no.10, pp.908 - 912
- Indexed
- SCIE
SCOPUS
- Journal Title
- ACS MEDICINAL CHEMISTRY LETTERS
- Volume
- 7
- Number
- 10
- Start Page
- 908
- End Page
- 912
- ISSN
- 1948-5875
- Abstract
- 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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