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: http://dx.doi.org/10.2174/1389557013406891

Publication date: 2001-09-01

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The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.