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. 2024-01-20T03:04:28Z 2024-01-20T03:04:28Z 2021-09-05 2016-10 1948-5875 https://pubs.kist.re.kr/handle/201004/123601 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. English AMER CHEMICAL SOC PI3K-GAMMA INHIBITION KINASE P110-DELTA POTENT MODELS 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 Article 10.1021/acsmedchemlett.6b00209 1 ACS MEDICINAL CHEMISTRY LETTERS, v.7, no.10, pp.908 - 912 ACS MEDICINAL CHEMISTRY LETTERS 7 10 908 912 scie scopus 000385689300009 2-s2.0-84991449945 Chemistry, Medicinal Pharmacology & Pharmacy Article PI3K-GAMMA INHIBITION KINASE P110-DELTA POTENT MODELS PI3K-delta PI3K-gamma phosphatidylinositol-4,5-bisphosphate 3-kinase-delta p110-delta p110-gamma kinase inhibitor