Preparation and biological activity of amino acid and peptide conjugates of antitumor hydroxymethylacylfulvene

The primary hydroxyl group in hydroxymethylacylfulvene, a potent antitumor drug, is readily replaced by thiols including cysteine, N-acetylcysteine, h omocysteine, and glutathione. Best yields are obtained when reaction is car ried out in the presence of dilute sulfuric acid. A variety of sulfur-conta ining analogues have been prepared, and their toxicity to tumor cells was e xamined.