The key role of hydroxylation for the cytostatic activity and selectivity of cyclophosphamide View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1984-06

AUTHORS

Peter Hilgard, Norbert Brock

ABSTRACT

The "pro-drug" cyclophosphamide (CP) is activated by liver "mixed function" hydroxylases to 4-hydroxy-cyclophosphamide (4-OH-CP), which represents the cytostatically active principle. Since the primary metabolite 4-OH-CP retains all the specific pharmacological properties of the parent compound without the need of metabolic activation, it constituted the basic principle and rationale for further drug development. Due to its chemical instability, 4-OH-CP had to be stabilized through appropriate substitutions at the 4-position of the oxazaphosphorine ring. ASTA Z 7557, in which the side chain is a 2-mercapto-ethanesulfonate, represents the prototype of this new class of oxazaphosphorines. More... »

PAGES

131-132

References to SciGraph publications

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/bf00232341

DOI

http://dx.doi.org/10.1007/bf00232341

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1052074757

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/6469505


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