BLEDTA II: Synthesis of a new tumor-visualizing derivative of Co(III)-bleomycin

L. H. DeRiemer, C. F. Meares, D. A. Goodwin, C. I. Diamanti

Research output: Contribution to journalArticlepeer-review

68 Scopus citations

Abstract

A new bifunctional chelating agent, (S)-1-(p-bromoacetamidobenzyl) ethylenedinitrilotetraacetic acid, has been prepared from L-phenylalanine. Reaction of the chelating agent with the Co(III) complex of the antitumor antibody bleomycin-A2DM was used to generate a new derivative of Co(III)-bleomyin, BLEDTA II. The product can be radiolabeled quickly by binding a radioactive metal ion to the EDTA group. The in vivo distribution of 111In-BLEDTA II in tumor-bearing mice was determined and found to be indistinguishable from that of the clinically useful 111In(III)-BLEDTA I complex.

Original languageEnglish (US)
Pages (from-to)1517-1534
Number of pages18
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume18
Issue number10
StatePublished - 1981

ASJC Scopus subject areas

  • Clinical Biochemistry
  • Molecular Medicine
  • Analytical Chemistry
  • Organic Chemistry
  • Drug Discovery
  • Pharmacology

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