Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation.

Md Saifuzzaman,Rick Morrison,Zhaohua Zheng,Stephanie Orive,Justin Hamilton,Philip E Thompson,Jasim M A Al-Rawi

Bioorganic & Medicinal Chemistry（2017）

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摘要

•Synthesis of 40 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones.•Atropisomers of O-substituted-8-aryl-copounds resulted from hindered rotation.•Bulky substitutions impeded binding except in the case of PI3Kδ and PDE3.•Piperazinyl 26a showed ADP-induced platelet-rich plasma aggregation (IC50 of 10μM).

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Synthesis of O-substituted-2-morpholino-8-aryl-benzo-oxazin-4-one,DNA-PK,PI3K,PDE3A,Antiplatelet activity

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