Journal article
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives
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 …
Authors
Clapham KM; Rennison T; Jones G; Craven F; Bardos J; Golding BT; Griffin RJ; Haggerty K; Hardcastle IR; Thommes P
Journal
Organic & Biomolecular Chemistry, Vol. 10, No. 33, pp. 6747–6757
Publisher
Royal Society of Chemistry (RSC)
Publication Date
2012
DOI
10.1039/c2ob26035b
ISSN
1477-0520