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Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives

Lookup NU author(s): Dr Tommy Rennison, Faye Craven, Emeritus Professor Bernard Golding, Professor Roger Griffin, Dr Karen Haggerty, Dr Ian HardcastleORCiD, Dr Celine CanoORCiD


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Substitution at the 7-position of the chromen-4-one pharmacophore 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 allyl, n-propyl or methyl enabled the resolution by chiral HPLC of atropisomers. Biological evaluation against DNA-PK of each pair of atropisomers showed a marked difference in potency, with biological activity residing exclusively in the laevorotatory enantiomer.

Publication metadata

Author(s): Clapham KM, Rennison T, Jones G, Craven F, Bardos J, Golding BT, Griffin RJ, Haggerty K, Hardcastle IR, Thommes P, Ting A, Cano C

Publication type: Article

Publication status: Published

Journal: Organic & Biomolecular Chemistry

Year: 2012

Volume: 10

Issue: 33

Pages: 6747-6757

Print publication date: 16/07/2012

ISSN (print): 1477-0520

ISSN (electronic): 1477-0539

Publisher: Royal Society of Chemistry


DOI: 10.1039/c2ob26035b


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