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8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) |
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| Authors: | Desage-El Murr Marine Cano Celine Golding Bernard T Hardcastle Ian R Hummersome Marc Frigerio Mark Curtin Nicola J Menear Keith Richardson Caroline Smith Graeme C M Griffin Roger J |
| Institution: | aNorthern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne NE1 7RU, UK;bKuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0PE, UK |
| 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. |
| Keywords: | DNA-PK Kinase inhibitor DNA-repair Chromenones Cancer |
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