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J Med Chem. 2000 Sep 21;43(19):3577-80.

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

Author information

1
Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093-0506, USA.

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.

PMID:
11000013
DOI:
10.1021/jm0000315
[Indexed for MEDLINE]

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