The metabolism and antitumour activity of the enantiomers of cis- and trans-4-methylcyclophosphamide.
Chem Biol Interact
; 18(1): 47-57, 1977 Jul.
Article
em En
| MEDLINE
| ID: mdl-890840
ABSTRACT
4-Methylcyclophosphamide, an analogue of the antitumour agent cyclophosphamide, exists in cis and trans forms, each of which comprises a pair of optical isomers. The extents of metabolism by rat liver microsomes during 20 min were compared for the four steroisomers incubated separately, and for the racemic cis and trans-derivatives in admixture, using mass spectrometry and gas chromatography respectively. In comparative antitumour tests against the ADJ/PC6 plasma cell tumour in mice, the racemic cis and trans forms of 4- and 6-methylcyclophosphamide had similar therapeutic indices. The four stereoisomers of 4-methylcyclophosphamide exhibited an approx. two-fold range in therapeutic index so that there was no marked effect on either metabolism or antitumour activity occasioned by change of configuration either at C-4 or at phosphorus.
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Base de dados:
MEDLINE
Assunto principal:
Ciclofosfamida
/
Antineoplásicos
Limite:
Animals
Idioma:
En
Ano de publicação:
1977
Tipo de documento:
Article