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
DC Field | Value | Language |
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dc.contributor.author | Ferguson, Fleur M. | - |
dc.contributor.author | Ni, Jing | - |
dc.contributor.author | Zhang, Tinghu | - |
dc.contributor.author | Tesar, Bethany | - |
dc.contributor.author | Sim, Taebo | - |
dc.contributor.author | Kim, Nam Doo | - |
dc.contributor.author | Deng, Xianming | - |
dc.contributor.author | Brown, Jennifer R. | - |
dc.contributor.author | Zhao, Jean J. | - |
dc.contributor.author | Gray, Nathanael S. | - |
dc.date.accessioned | 2021-09-03T19:27:40Z | - |
dc.date.available | 2021-09-03T19:27:40Z | - |
dc.date.created | 2021-06-16 | - |
dc.date.issued | 2016-10 | - |
dc.identifier.issn | 1948-5875 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/87371 | - |
dc.description.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. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.subject | PI3K-GAMMA INHIBITION | - |
dc.subject | KINASE | - |
dc.subject | P110-DELTA | - |
dc.subject | POTENT | - |
dc.subject | MODELS | - |
dc.title | 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 | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Sim, Taebo | - |
dc.identifier.doi | 10.1021/acsmedchemlett.6b00209 | - |
dc.identifier.scopusid | 2-s2.0-84991449945 | - |
dc.identifier.wosid | 000385689300009 | - |
dc.identifier.bibliographicCitation | ACS MEDICINAL CHEMISTRY LETTERS, v.7, no.10, pp.908 - 912 | - |
dc.relation.isPartOf | ACS MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.title | ACS MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 7 | - |
dc.citation.number | 10 | - |
dc.citation.startPage | 908 | - |
dc.citation.endPage | 912 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.subject.keywordPlus | PI3K-GAMMA INHIBITION | - |
dc.subject.keywordPlus | KINASE | - |
dc.subject.keywordPlus | P110-DELTA | - |
dc.subject.keywordPlus | POTENT | - |
dc.subject.keywordPlus | MODELS | - |
dc.subject.keywordAuthor | PI3K-delta | - |
dc.subject.keywordAuthor | PI3K-gamma | - |
dc.subject.keywordAuthor | phosphatidylinositol-4,5-bisphosphate 3-kinase-delta | - |
dc.subject.keywordAuthor | p110-delta | - |
dc.subject.keywordAuthor | p110-gamma | - |
dc.subject.keywordAuthor | kinase inhibitor | - |
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