Synthesis and biological evaluation of a novel decadentate ligand DEPA.
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.
Chong
Hyun-Soon
HS
Physical Sciences Department, Illinois Institute of Technology, LS 182, Chicago, IL 60616, USA. Chong@iit.edu
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
D002614:Chelating Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis* / Q000494:pharmacology*; D008024:Ligands; D015203:Reproducibility of Results
C545867:7-(2-(bis-carboxymethyl-amino)ethyl)-4,10-bis-carboxymethyl-1,4,7,10-tetraazacyclododec-1-yl-acetic acid; D002614:Chelating Agents; D006573:Heterocyclic Compounds, 1-Ring; D008024:Ligands; D005998:Glycine