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

  • Bioorg Med Chem Lett. 2010 Jun 15;20(12):3649-53. doi: 10.1016/j.bmcl.2010.04.102.
Sara L Payne  1 ,  Sonsoles Rodriguez-Aristegui ,  Julia Bardos ,  Céline Cano ,  Bernard T Golding ,  Ian R Hardcastle ,  Marcus Peacock ,  Nahida Parveen ,  Roger J Griffin
Affiliations
  • 1. Northern Institute for Cancer Research, School of Chemistry, Newcastle University, Newcastle Upon Tyne, UK.
PMID: 20472428 DOI: 10.1016/j.bmcl.2010.04.102
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.

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