Send to

Choose Destination
Bioorg Med Chem. 1995 Oct;3(10):1299-304.

Conjugation of doxorubicin to monoclonal anti-carcinoembryonic antigen antibody via novel thiol-directed cross-linking reagents.

Author information

School of Pharmacy, Memorial University of Newfoundland, St John's, Canada.


In order to improve the available methods to produce an immunoconjugate the use of longer heterobifunctional cross-linking reagents were investigated. Two new maleimidobenzoyl spacers have been synthesized in a one step process from 4-maleimidobenzoic acid. The new heterobifunctional cross-linking reagents were fully characterized by their IR, 1H NMR, 13C NMR and mass spectra. These spacers are selectively attached to NH2-3' of the daunosamine moiety of doxorubicin. The spacer-doxorubicin derivatives were also characterized by 1H NMR spectrometry before coupling to thiol groups of thiolated anti-carcinoembryonic antigen (CEA) monoclonal antibody (11-285-14). These conjugates contain 1.51-3.44 molecules of drug for each molecule of monoclonal antibody (MAb).

[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center