3986-06-9Relevant academic research and scientific papers
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives
Clapham, Kate M.,Rennison, Tommy,Jones, Gavin,Craven, Faye,Bardos, Julia,Golding, Bernard T.,Griffin, Roger J.,Haggerty, Karen,Hardcastle, Ian R.,Thommes, Pia,Ting, Attilla,Cano, Céline
experimental part, p. 6747 - 6757 (2012/09/22)
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.
