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Synthesis and biological evaluation of a novel decadentate ligand DEPA.

ABSTRACT: An efficient and short synthetic route to a novel decadentate ligand 7-[2-(bis-carboxymethyl-amino)-ethyl]-4,10-bis-carboxymethyl-1,4,7,10-tetraaza-cyclododec-1-yl-acetic acid (DEPA) with both macrocyclic and acyclic binding moieties is reported. A reproducible and scalable synthetic method to a precursor molecule of DEPA, 1,4,7-tris(tert-butoxycarbonylmethyl)tetraazacyclododecane was developed. DEPA was evaluated as a chelator of (177)Lu, (212)Bi, and (213)Bi for potential use in an antibody-targeted cancer therapy, radioimmunotherapy (RIT) using Arsenazo III based spectroscopic complexation kinetics, in vitro serum stability, and in vivo biodistribution studies.

SUBMITTER: Chong HS

PROVIDER: S-EPMC2784163 | biostudies-literature | 2008 Nov

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of a novel decadentate ligand DEPA.

Chong Hyun-Soon HS Lim Sooyoun S Baidoo Kwamena E KE Milenic Diane E DE Ma Xiang X Jia Fang F Song Hyun A HA Brechbiel Martin W MW Lewis Michael R MR

Bioorganic & medicinal chemistry letters 20080919 21

An efficient and short synthetic route to a novel decadentate ligand 7-[2-(bis-carboxymethyl-amino)-ethyl]-4,10-bis-carboxymethyl-1,4,7,10-tetraaza-cyclododec-1-yl-acetic acid (DEPA) with both macrocyclic and acyclic binding moieties is reported. A reproducible and scalable synthetic method to a precursor molecule of DEPA, 1,4,7-tris(tert-butoxycarbonylmethyl)tetraazacyclododecane was developed. DEPA was evaluated as a chelator of (177)Lu, (212)Bi, and (213)Bi for potential use in an antibody-ta ...[more]

PMID: 18845437

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