Indolequinone antitumor agents: relationship between quinone structure and rate of metabolism by recombinant human NQO1.

Abstract

A series of indolequinones bearing various functional groups has been synthesized, and the effects of substituents on the metabolism of the quinones by recombinant human NAD(P)H:quinone oxidoreductase (NQO1), and on the toxicity toward nonsmall cell lung cancer cells with either high NQO1 activity (H460) or with no detectable activity (H596) were studied.

• Authors: H D Beall, A R Hudnott, S Winski, D Siegel, E Swann, D Ross, C J Moody
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 8 Issue 5 Pg. 545-8 (Mar 03 1998) ISSN: 0960-894X [Print] England
• PMID: 9871615 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antineoplastic Agents
• Quinones
• Recombinant Proteins
• NAD(P)H Dehydrogenase (Quinone)

Topics

• Antineoplastic Agents (chemistry, metabolism)
• Carcinoma, Small Cell (enzymology, pathology)
• Humans
• Kinetics
• Lung Neoplasms (enzymology, pathology)
• NAD(P)H Dehydrogenase (Quinone) (metabolism)
• Quinones (chemistry, metabolism)
• Recombinant Proteins (metabolism)
• Structure-Activity Relationship
• Tumor Cells, Cultured