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ID: ALA1157906

Journal: Bioorg Med Chem Lett

Title: Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2.

Authors: Nolan KA, Humphries MP, Bryce RA, Stratford IJ.

Abstract: The purpose of the work was to identify novel inhibitors of the enzyme NQO2. Using computational molecular modelling, a QSAR (R(2)=0.88) was established, relating inhibitory potency with calculated binding affinity. From this, the imidazoacridin-6-one, NSC660841, was identified as the most potent inhibitor of NQO2 yet reported (IC(50)=6 nM).

CiteXplore: 20356739

DOI: 10.1016/j.bmcl.2010.03.051