Synthesis and biological evaluation of a novel decadentate ligand DEPA |
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Authors: | Chong Hyun-Soon Lim Sooyoun Baidoo Kwamena E Milenic Diane E Ma Xiang Jia Fang Song Hyun A Brechbiel Martin W Lewis Michael R |
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Affiliation: | Physical Sciences Department, Illinois Institute of Technology, LS 182, Chicago, IL 60616, USA. Chong@iit.edu |
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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. |
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