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Issue 33, 2012
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Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives

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Abstract

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.

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

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Publication details

The article was received on 29 May 2012, accepted on 12 Jul 2012, published on 16 Jul 2012 and first published online on 16 Jul 2012


Article type: Paper
DOI: 10.1039/C2OB26035B
Citation: Org. Biomol. Chem., 2012,10, 6747-6757
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    Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives

    K. M. Clapham, T. Rennison, G. Jones, F. Craven, J. Bardos, B. T. Golding, R. J. Griffin, K. Haggerty, I. R. Hardcastle, P. Thommes, A. Ting and C. Cano, Org. Biomol. Chem., 2012, 10, 6747
    DOI: 10.1039/C2OB26035B

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