1275599-68-2Relevant articles and documents
DNA-dependent protein kinase (DNA-PK) inhibitors: Structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain
Clapham, Kate M.,Bardos, Julia,Finlay, M. Raymond V.,Golding, Bernard T.,Griffen, Edward J.,Griffin, Roger J.,Hardcastle, Ian R.,Menear, Keith A.,Ting, Attilla,Turner, Paul,Young, Gail L.,Cano, Céline
experimental part, p. 966 - 970 (2011/03/20)
Introduction of an O-alkoxyphenyl substituent at the 8-position of the 2-morpholino-4H-chromen-4-one pharmacophore enabled regions of the ATP-binding site of DNA-dependent protein kinase (DNA-PK) to be probed further. Structure-activity relationships have been elucidated for inhibition of DNA-PK and PI3K (p110α), with N-(2-(cyclopropylmethoxy)-4-(2-morpholino-4-oxo-4H- chromen-8-yl)phenyl)-2-morpholinoacetamide 11a being identified as a potent and selective DNA-PK inhibitor (IC50 = 8 nM).
