8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
The synthesis and biological evaluation of libraries of 8-biarylchromen-4-ones enabled the elucidation of structure-activity relationships for inhibition of the DNA-dependent protein kinase (DNA-PK), with 8-(3-(thiophen-2-yl)phenyl)chromen-4-one and 8-(3-(thiophen-3-yl)phenyl)chromen-4-one being especially potent inhibitors.
Desage-El Murr
Marine
M
Northern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne NE1 7RU, UK.
Cano
Celine
C
Golding
Bernard T
BT
Hardcastle
Ian R
IR
Hummersome
Marc
M
Frigerio
Mark
M
Curtin
Nicola J
NJ
Menear
Keith
K
Richardson
Caroline
C
Smith
Graeme C M
GC
Griffin
Roger J
RJ
D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051747:DNA-Activated Protein Kinase / Q000037:antagonists & inhibitors*; D006367:HeLa Cells; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D002867:Chromones; D047428:Protein Kinase Inhibitors; D011838:Radiation-Sensitizing Agents; D051747:DNA-Activated Protein Kinase