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Synthesis, antibody conjugation, radiolabeling, and biodistribution of the first diethylene triamine pentahydroxamate (DTPH) bifunctional chelating agent
Author(s) -
Safavy A.,
Smith D. C.,
Bazooband A.,
Buchsbaum D. J.
Publication year - 2001
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.25804401260
Subject(s) - chemistry , conjugate , biodistribution , bifunctional , hydrazide , chelation , conjugated system , yield (engineering) , combinatorial chemistry , stereochemistry , organic chemistry , catalysis , in vitro , biochemistry , mathematical analysis , polymer , materials science , mathematics , metallurgy
Abstract Synthesis of a novel pentahydroxamic acid bifunctional chelating agent (BCA) constructed on the diethylene triamine core of diethylene triamine pentaacetic acid (DTPA) is reported. Thus, the N α , N ζ ‐[tetrakis((N‐hydroxy‐N‐methyl)carbonyl)]‐N 4 ‐[((N‐hydroxy‐N‐methyl)carbonyl)]‐4‐(2, 6‐diamino)‐4‐azahexanoic hydrazide (DTPH, 1) was synthesized through a convergent synthetic strategy, in 14 steps and in 8% overall yield. The BCA was conjugated to the monoclonal antibody (MAb) ?CH2HuCC49 and the conjugate was radiolabeled with 177 Lu. Results of biodistribution of this labeled conjugate in athymic nude mice are reported.