Benzofuran-, benzothiophene-, indazole- and benzisoxazole-quinones: Excellent substrates for NAD(P)H:quinone oxidoreductase 1 |
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| Authors: | Jeffery J Newsome Mary Hassani Elizabeth Swann Jane M Bibby Howard D Beall Christopher J Moody |
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| Institution: | 1. Department of Chemistry, University of Exeter, Stocker Road, Exeter EX4 4QD, UK;2. Department of Biomedical and Pharmaceutical Sciences, The University of Montana, 32 Campus Drive #1552, Missoula, MT 59812-1552, USA;3. School of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, UK |
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| Abstract: | A series of heterocyclic quinones based on benzofuran, benzothiophene, indazole and benzisoxazole has been synthesized, and evaluated for their ability to function as substrates for recombinant human NAD(P)H:quinone oxidoreductase (NQO1), a two-electron reductase upregulated in tumor cells. Overall, the quinones are excellent substrates for NQO1, approaching the reduction rates observed for menadione. |
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| Keywords: | Quinone Benzofuran Benzothiophene Indazole Quinone reductase NQO1 |
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