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.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Farmer PB,Jarman M,Facchinetti T,Pankiewicz K,Stec WJdoi
10.1016/0009-2797(77)90140-5subject
Has Abstractpub_date
1977-07-01 00:00:00pages
47-57issue
1eissn
0009-2797issn
1872-7786pii
0009-2797(77)90140-5journal_volume
18pub_type
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