2. Academic Validation
  3. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries

Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries

  • Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. doi: 10.1016/j.bmcl.2004.09.060.
Justin J J Leahy 1,  Bernard T Golding,  Roger J Griffin,  Ian R Hardcastle,  Caroline Richardson,  Laurent Rigoreau,  Graeme C M Smith
Affiliations

Affiliation

  • 1 Northern Institute for Cancer Research, School of Natural Sciences-Chemistry, Bedson Building, University of Newcastle, Newcastle Upon Tyne NE1 7RU, UK.
PMID: 15546735 DOI: 10.1016/j.bmcl.2004.09.060
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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