Drug metabolism and disposition : the biological fate of chemicals
The most recent articles from:
September 1999
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Drug Metab. Dispos. · Sep 1999
Metabolism of antitumor hydroxymethylacylfulvene by rat liver cytosol.
Acylfulvenes are a potent class of antitumor agents derived from illudin S, a fungal sesquiterpene. Illudin S possesses antitumor activity but has a poor therapeutic index. Acylfulvene is 100-fold less toxic against human lung adenocarcinoma cells than illudin S, but inhibits tumor growth in human xenografts, opposite to illudin S. ⋯ However, the reaction occurred more slowly. In addition, four new metabolites were isolated, two hydroxylated derivatives and two in which the primary allylic hydroxyl was replaced by hydride. All retained the reactive centers of the parent MGI 114.