Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives |
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| Authors: | Kate M Clapham Tommy Rennison Gavin Jones Faye Craven Julia Bardos Bernard T Golding Roger J Griffin Karen Haggerty Ian R Hardcastle Pia Thommes Attilla Ting Céline Cano |
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| Affiliation: | Newcastle Cancer Centre, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle upon Tyne, NE1 7RU, UK. celine.cano@ncl.ac.uk. |
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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. |
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