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.
Physical Sciences Department, Illinois Institute of Technology, LS 182, Chicago, IL 60616, USA. Chong@iit.edu
Hyun-Soon
HS
Chong
Sooyoun
S
Lim
Kwamena E
KE
Baidoo
Diane E
DE
Milenic
Xiang
X
Ma
Fang
F
Jia
Hyun A
HA
Song
Martin W
MW
Brechbiel
Michael R
MR
Lewis
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