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Formation of the Cytotoxic Aldehyde Acrolein during in vitro Degradation of Cyclophosphamide

Nature New Biology volume 233, pages 250–252 (1971)Cite this article

Abstract

CYCLOPHOSPHAMIDE (I), the widely used antitumour agent synthesized by Arnold and Bourseaux1, has to be biologically converted into an active compound for it to be effective in vivo1–7. This activation takes place preferentially in the liver4, more specifically in its microsomes in the presence of NADPH and oxygen6 by means of the mixed function oxidase system7,8. Brock and Hohorst7 assumed that the cyclophosphamide ring opened by N-dealkylation or O-dealkylation to give primary active metabolites. Norpoth et al.9 favoured O-dealkylation as the mechanism leading to the production of the active transformation product.

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Authors and Affiliations

  1. Children's Cancer Research Foundation, and Departments of Pathology and Biological Chemistry, Harvard Medical School, Boston, Massachusetts, 02115

    R. A. ALARCON & J. MEIENHOFER

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  1. R. A. ALARCON
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  2. J. MEIENHOFER
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ALARCON, R., MEIENHOFER, J. Formation of the Cytotoxic Aldehyde Acrolein during in vitro Degradation of Cyclophosphamide. Nature New Biology 233, 250–252 (1971). https://doi.org/10.1038/newbio233250b0

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