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Bioorg Med Chem Lett. 2010 May 1;20(9):2832-6. doi: 10.1016/j.bmcl.2010.03.051. Epub 2010 Mar 15.

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

Author information

1
School of Pharmacy and Pharmaceutical Sciences, the University of Manchester and Manchester Cancer Research Center, Oxford Road, Manchester M13 9PT, UK.

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).

PMID:
20356739
DOI:
10.1016/j.bmcl.2010.03.051
[Indexed for MEDLINE]

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