Biologic Activity of Daunorubicin Linked to Proteins via the Methylketone Side Chain
Open Access
- 1 December 1981
- journal article
- research article
- Published by SAGE Publications in Tumori Journal
- Vol. 67 (6) , 521-524
- https://doi.org/10.1177/030089168106700602
Abstract
New daunorubicin-protein conjugates were prepared by covalently linking the antitumor drug to various test proteins via its methylketone side chain. Attachment of daunorubicin to proteins was achieved by nucleophylic substitution reaction of the 14-bromo derivative of the drug, under mild coupling conditions. In contrast to conventional methods, this procedure did not involve reaction or modification of the amino sugar. As expected, the covalent linkage of the drug was generally associated with an appreciable reduction in the drug cytotoxicity to HeLa cells in vitro. The possible advantages of this method for coupling to specific protein carriers are discussed.This publication has 13 references indexed in Scilit:
- Studies on amino acid and peptide derivatives of daunorubicineFEBS Letters, 1979
- Increased selectivity of drugs by linking to carriersPublished by Elsevier ,1978
- The use of macromolecules as carriers of antitumor drugsPublished by Elsevier ,1977
- Melanotropin–daunomycin conjugate shows receptor-mediated cytotoxicity in cultured murine melanoma cellsNature, 1977
- The interaction of adriamycin and its β anomer with DNABiochimica et Biophysica Acta (BBA) - Nucleic Acids and Protein Synthesis, 1977
- Targeting of drugsNature, 1977
- Concanavalin A as a carrier of daunomycinNature, 1977
- Steric influence of the orientation of the primary amino group at position 3 of the sugar moiety of anthracycline antibiotics in DNA binding propertiesCancer Letters, 1977
- Synthesis and biological evaluation of some 14-O-acyl derivatives of adriamycinJournal of Medicinal Chemistry, 1974
- Interaction of daunomycin and its derivatives with DNABiochimica et Biophysica Acta (BBA) - Nucleic Acids and Protein Synthesis, 1972