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Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives
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
Institution: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.
Abstract:Substitution at the 7-position of the chromen-4-one pharmacophore of 8-(dibenzob,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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