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Bledta II: Synthesis of a new tumor‐visualizing derivative of CO(III)‐bleomycin
Author(s) -
Deriemer Leslie H.,
Meares Claude F.,
Goodwin David A.,
Diamanti Carol I.
Publication year - 1981
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580181017
Subject(s) - chemistry , bleomycin , bifunctional , chelation , derivative (finance) , in vivo , stereochemistry , phenylalanine , metal , combinatorial chemistry , radiochemistry , biochemistry , organic chemistry , amino acid , chemotherapy , medicine , surgery , microbiology and biotechnology , financial economics , economics , biology , catalysis
A new bifunctional chelating agent, (S)‐l‐(p‐bromoacetamidobenzyl) ethylenedinitrilotetraacetic acid, has been prepared from L‐phenylalanine. Reaction of the chelating agent with the Co(III) complex of the antitumor antibiotic bleomycin‐A 2 DM was used to generate a new derivative of Co(III)‐bleomycin, BLEDTA II. The product can be radiolabeled quickly by binding a radioactive metal ion to the EDTA group. The in vivo distribution of 111 In‐BLEDTA II in tumor‐bearing mice was determined and found to be indistinguishable from that of the clinically useful 111 In(III)‐BLEDTA I complex (J. Med. Chem. 22 : 1019 (1979)).