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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| 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 |
| ISSN (print) | | 1477-0520 |
| ISSN (electronic) | | 1477-0539 |
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| Full text for this publication is not currently held within this repository. Alternative links are provided below where available. |
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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. |
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| Publisher | | Royal Society of Chemistry |
| URL | | http://dx.doi.org/10.1039/b926245h |
| DOI | | 10.1039/b926245h |
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