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, 14 (24), 6083-7

Identification of a Highly Potent and Selective DNA-dependent Protein Kinase (DNA-PK) Inhibitor (NU7441) by Screening of Chromenone Libraries

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Identification of a Highly Potent and Selective DNA-dependent Protein Kinase (DNA-PK) Inhibitor (NU7441) by Screening of Chromenone Libraries

Justin J J Leahy et al. Bioorg Med Chem Lett.

Abstract

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 repair enzyme DNA-dependent protein kinase (DNA-PK). These studies resulted in the identification of 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one (NU7441) as a highly potent and selective DNA-PK inhibitor (IC50=14 nM), exhibiting ATP-competitive inhibition kinetics.

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