Abstract:
:The cancer chemotherapeutic drug, 5-(3,3-dimethyl-1-triazeno) imidazole-4-carboxamide (DIC, DTIC, NSC-45388), is metabolised in rats to a structurally related product which was detected by thin-layer chromatography. The novel metabolite has a lower mobility and a colour reaction that is indistinguishable from the parent compound. The metabolite is not retained on an anionic exchanger which is inconsistent with the expected covalent binding of the drug to endogenic anionic substrates (e.g. glucuronic acid). Since both DIC and the metabolite yielded 5-[(4-ethylamino-1-napthyl)-azo]imidazole-4-carboxamide through release of 5-diazoimidazole-4-carboxamide, followed by coupling with N-ethyl-1-napthylamine, no biotransformation (hydroxylation) of the imidazole moiety of the injected DIC had occurred. By corollary, the lowered chromatographic mobility of the metabolite was explicable by the introduction of a polar but non-acidic function into the terminal dimethylamino group of the triazene side-chain. The metabolite was identified as 5-(3-hydroxymethyl-3-methyl-1-triazeno)imidazole-4-carboxamide by co-chromatography with an authentic sample of HMIC and by its methylating capacity for nucleophilic substrates.
journal_name
Cancer Lettjournal_title
Cancer lettersauthors
Kolar GF,Maurer M,Wildschütte Mdoi
10.1016/0304-3835(80)90076-2subject
Has Abstractpub_date
1980-09-01 00:00:00pages
235-41issue
3eissn
0304-3835issn
1872-7980pii
0304-3835(80)90076-2journal_volume
10pub_type
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