Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin-and isocoumarin-derived inhibitors

SL Payne, S Rodriguez-Aristegui, J Bardos…

Index: Payne, Sara L.; Rodriguez-Aristegui, Sonsoles; Bardos, Julia; Cano, Celine; Golding, Bernard T.; Hardcastle, Ian R.; Peacock, Marcus; Parveen, Nahida; Griffin, Roger J. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 12 p. 3649 - 3653

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Citation Number: 10

Abstract

Replacement of the core heterocycle of a defined series of chromen-4-one DNA-PK inhibitors by the isomeric chromen-2-one (coumarin) and isochromen-1-one (isocoumarin) scaffolds was investigated. Structure–activity relationships for DNA-PK inhibition were broadly consistent, albeit with a reduction of potency compared with the parent chromenone.