title: 8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
abstract: 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.
authors.affiliation: Northern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne NE1 7RU, UK.
authors.forename: Marine
authors.initials: M
authors.lastname: Desage-El Murr
authors.forename: Celine
authors.initials: C
authors.lastname: Cano
authors.forename: Bernard T
authors.initials: BT
authors.lastname: Golding
authors.forename: Ian R
authors.initials: IR
authors.lastname: Hardcastle
authors.forename: Marc
authors.initials: M
authors.lastname: Hummersome
authors.forename: Mark
authors.initials: M
authors.lastname: Frigerio
authors.forename: Nicola J
authors.initials: NJ
authors.lastname: Curtin
authors.forename: Keith
authors.initials: K
authors.lastname: Menear
authors.forename: Caroline
authors.initials: C
authors.lastname: Richardson
authors.forename: Graeme C M
authors.initials: GC
authors.lastname: Smith
authors.forename: Roger J
authors.initials: RJ
authors.lastname: Griffin
mesh_terms: 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
chemical_list: D002867:Chromones; D047428:Protein Kinase Inhibitors; D011838:Radiation-Sensitizing Agents; D051747:DNA-Activated Protein Kinase