Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK)

  1. Lookup NU author(s)
  2. Dr Celine Cano
  3. Professor Bernard Golding
  4. Dr Karen Haggerty
  5. Dr Ian Hardcastle
  6. Professor Roger Griffin
Author(s)Cano C, Golding BT, Haggerty K, Hardcastle IR, Peacock M, Griffin RJ
Publication type Article
JournalOrganic & Biomolecular Chemistry
ISSN (print)1477-0520
ISSN (electronic)1477-0539
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Substitution at the 3-position of the dibenzothiophen-4-yl ring of 8-(dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-one NU7441, a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor, with propyl, allyl or methyl enabled the separation by chiral HPLC of atropisomers. This is a consequence of restricted rotation about the dibenzothiophene–chromenone bond. Biological evaluation against DNA-PK of the pairs of atropisomers showed a marked difference in potency, with only one enantiomer being biologically active.
PublisherRoyal Society of Chemistry
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