Abstract
N-Oxide-containing compounds have been developed as prodrugs that are selectively bioactivated in the hypoxic cells in tumors. This selectivity is based on the net reduction of the N-oxide moiety in the absence of oxygen, in a one or two-electron process, by reductive enzymes. A wide range of N-oxides have been studied and some of them are currently in clinical use. This review covers the principal families of compounds under study and in clinical trials.
Keywords: N-Oxides, Hypoxia, Cytotoxins, Tumor Hypoxia, Bioreductive Agents, Imidazopyridopyrazine N-Oxide and Imidazoquin-oxaline N-Oxide, Quinoxaline N,N-Dioxide, Aminoalkylaminoanthraquinone N-Oxide, Aminoalkylaminoacridine N-Oxide
Mini-Reviews in Medicinal Chemistry
Title: N-Oxides as Hypoxia Selective Cytotoxins
Volume: 1 Issue: 3
Author(s): Hugo Cerecetto and Mercedes Gonzalez
Affiliation:
Keywords: N-Oxides, Hypoxia, Cytotoxins, Tumor Hypoxia, Bioreductive Agents, Imidazopyridopyrazine N-Oxide and Imidazoquin-oxaline N-Oxide, Quinoxaline N,N-Dioxide, Aminoalkylaminoanthraquinone N-Oxide, Aminoalkylaminoacridine N-Oxide
Abstract: N-Oxide-containing compounds have been developed as prodrugs that are selectively bioactivated in the hypoxic cells in tumors. This selectivity is based on the net reduction of the N-oxide moiety in the absence of oxygen, in a one or two-electron process, by reductive enzymes. A wide range of N-oxides have been studied and some of them are currently in clinical use. This review covers the principal families of compounds under study and in clinical trials.
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Cite this article as:
Cerecetto Hugo and Gonzalez Mercedes, N-Oxides as Hypoxia Selective Cytotoxins, Mini-Reviews in Medicinal Chemistry 2001; 1 (3) . https://dx.doi.org/10.2174/1389557013406891
DOI https://dx.doi.org/10.2174/1389557013406891 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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