N-Oxides as Hypoxia Selective Cytotoxins

Authors: Cerecetto H.; Gonzalez M.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 3, September 2001 , pp. 219-231(15)

Publisher: Bentham Science Publishers

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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-oxal; Quinoxaline N,N-Dioxide; Aminoalkylaminoanthraquinone N-Oxide; Aminoalkylaminoacridine N-Oxide

Language: English

Document Type: Review article

DOI: 10.2174/1389557013406891

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