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

Lookup NU author(s): Dr Celine Cano, Professor Bernard Golding, Dr Karen Haggerty, Dr Ian Hardcastle, Professor Roger Griffin

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Abstract

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.


Publication metadata

Author(s): Cano C, Golding BT, Haggerty K, Hardcastle IR, Peacock M, Griffin RJ

Publication type: Article

Journal: Organic & Biomolecular Chemistry

Year: 2010

Volume: 8

Issue: 8

Pages: 1922-1928

Print publication date: 01/01/2010

ISSN (print): 1477-0520

ISSN (electronic): 1477-0539

Publisher: Royal Society of Chemistry

URL: http://dx.doi.org/10.1039/b926245h

DOI: 10.1039/b926245h


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