2, 6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK)

JJ Hollick, BT Golding, IR Hardcastle, N Martin…

文献索引：Hollick, Jonathan J.; Golding, Bernard T.; Hardcastle, Ian R.; Martin, Niall; Richardson, Caroline; Rigoreau, Laurent J. M.; Smith, Graeme C. M.; Griffin, Roger J. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 18 p. 3083 - 3086

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被引用次数: 92

摘要

6-Aryl-2-morpholin-4-yl-4H-pyran-4-ones and 6-aryl-2-morpholin-4-yl-4H-thiopyran-4-ones were synthesised and evaluated as potential inhibitors of the DNA repair enzyme DNA- dependent protein kinase (DNA-PK). Several compounds in each series exhibited superior activity to the chromenone LY294002, and were of comparable potency to the benzochromenone NU7026 (IC50= 0.23 μM). Importantly, members of both structural ...