Abstract
The primary hydroxyl group in hydroxymethylacylfulvene, a potent antitumor drug, is readily replaced by thiols including cysteine, N-acetylcysteine, homocysteine, and glutathione. Best yields are obtained when reaction is carried out in the presence of dilute sulfuric acid. A variety of sulfur-containing analogues have been prepared, and their toxicity to tumor cells was examined.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acids / chemistry*
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Drug Screening Assays, Antitumor
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Inhibitory Concentration 50
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Peptides / chemistry*
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Rats
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Sesquiterpenes / chemistry*
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Sesquiterpenes / pharmacology
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Tumor Cells, Cultured
Substances
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Amino Acids
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Antineoplastic Agents
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Peptides
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Sesquiterpenes
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irofulven