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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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Article information


Submitted
29 May 2012
Accepted
12 Jul 2012
First published
16 Jul 2012

Org. Biomol. Chem., 2012,10, 6747-6757
Article type
Paper

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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