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Preparation and Biological Activity of Amino Acid and Peptide Conjugates of Antitumor Hydroxymethylacylfulvene
- Source :
- Journal of Medicinal Chemistry. 43:3577-3580
- Publication Year :
- 2000
- Publisher :
- American Chemical Society (ACS), 2000.
-
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.
- Subjects :
- chemistry.chemical_classification
Tetrapeptide
Antineoplastic Agents
Biological activity
Peptide
Glutathione
Chemical synthesis
Rats
Amino acid
Inhibitory Concentration 50
chemistry.chemical_compound
chemistry
Biochemistry
Drug Discovery
Tumor Cells, Cultured
Peptide synthesis
Animals
Molecular Medicine
Amino Acids
Drug Screening Assays, Antitumor
Peptides
Sesquiterpenes
Cysteine
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 43
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....601d7885d1718893972df417872f413d