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Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.
A solution-phase multiple-parallel synthesis approach was employed for the preparation of 6-, 7- and 8-aryl-substituted chromenone libraries, which were screened as inhibitors of the DNA repairExpand
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.
TLDR
Structure-activity relationships for inhibition of DNA-dependent protein kinase (DNA-PK) have been defined and a number of 7-alkoxy-substituted chromen-4-ones displayed improved activity. Expand
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in
TLDR
These structural classes were identified as novel DNA-PK inhibitors and delineated initial structure-activity relationships against DNA- PK, with only a 2-morpholino or 2-(2'-methyl morpholino) group being tolerated at this position. Expand