Benzimidazole- and benzothiazole-quinones: excellent substrates for NAD(P)H : quinone oxidoreductase 1

A series of benzimidazole-and benzothiazole-quinones has been synthesized. The ability of these heterocyclic quinones to act as substrates for recombinant human NAD(P)H:quinone oxidoreductase (NQO1), a two-electron reductase upregulated in tumour cells, was determined. Overall, the quinones were exc...

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Bibliographic Details
Published inOrganic & biomolecular chemistry Vol. 5; no. 22; pp. 3665 - 3673
Main Authors Newsome, Jeffery J., Colucci, Marie A., Hassani, Mary, Beall, Howard D., Moody, Christopher J.
Format Journal Article
LanguageEnglish
Published CAMBRIDGE Royal Soc Chemistry 01.01.2007
Subjects
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - metabolism
Benzothiazoles - chemical synthesis
Benzothiazoles - chemistry
Benzothiazoles - metabolism
Chemistry
Chemistry, Organic
Humans
Kinetics
NAD(P)H Dehydrogenase (Quinone) - metabolism
Physical Sciences
Quinones - chemical synthesis
Quinones - chemistry
Quinones - metabolism
Recombinant Proteins - metabolism
Science & Technology
Substrate Specificity
NQO1
IN-VITRO
NAD(P)H-QUINONE-OXIDOREDUCTASE-1
SERIES
DT-DIAPHORASE
ANALOGS
INDOLEQUINONE ANTITUMOR AGENTS
MECHANISM-BASED INHIBITOR
BIOREDUCTIVE ACTIVATION
STRUCTURE-METABOLISM
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Summary:A series of benzimidazole-and benzothiazole-quinones has been synthesized. The ability of these heterocyclic quinones to act as substrates for recombinant human NAD(P)H:quinone oxidoreductase (NQO1), a two-electron reductase upregulated in tumour cells, was determined. Overall, the quinones were excellent substrates for NQO1.
Bibliography:Medline
NIH RePORTER
ISSN:1477-0520
DOI:10.1039/b713044a