Lookup NU author(s): Dr Celine Cano,
Professor Bernard Golding,
Dr Karen Haggerty,
Dr Ian Hardcastle,
Professor Roger Griffin
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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.
Author(s): Cano C, Golding BT, Haggerty K, Hardcastle IR, Peacock M, Griffin RJ
Publication type: Article
Journal: Organic & Biomolecular Chemistry
Print publication date: 01/01/2010
ISSN (print): 1477-0520
ISSN (electronic): 1477-0539
Publisher: Royal Society of Chemistry
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