title: Preparation and biological activity of amino acid and peptide conjugates of antitumor hydroxymethylacylfulvene.
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.
authors.affiliation: Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093-0506, USA.
authors.forename: T C
authors.initials: TC
authors.lastname: McMorris
authors.forename: J
authors.initials: J
authors.lastname: Yu
authors.forename: H T
authors.initials: HT
authors.lastname: Ngo
authors.forename: H
authors.initials: H
authors.lastname: Wang
authors.forename: M J
authors.initials: MJ
authors.lastname: Kelner
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D010455:Peptides / Q000737:chemistry*; D051381:Rats; D012717:Sesquiterpenes / Q000737:chemistry* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
chemical_list: D000596:Amino Acids; D000970:Antineoplastic Agents; D010455:Peptides; D012717:Sesquiterpenes; C102714:irofulven