Efficient synthesis and evaluation of bimodal ligand NETA.
The efficient and short synthetic route to the structurally novel bimodal ligand NETA for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer was developed. The structure of NETA was determined by X-ray crystallography. The arsenazo-based UV spectroscopic complexation kinetics data suggest that NETA is a promising chelator for use in RIT applications of (212)Bi, (213)Bi, and (177)Lu.
Chong
Hyun-Soon
HS
Chemistry Division, Biological, Chemical, and Physical Sciences Department, Illinois Institute of Technology, 3101 S. Dearborn Street, LS 182, Chicago, IL 60616, USA. chong@iit.edu
Song
Hyun A
HA
Birch
Noah
N
Le
Thien
T
Lim
Sooyoun
S
Ma
Xiang
X
D000085:Acetates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001729:Bismuth; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D015195:Drug Design; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D008024:Ligands; D008187:Lutetium; D008968:Molecular Conformation; D015394:Molecular Structure; D016499:Radioimmunotherapy; D011868:Radioisotopes
C529856:(2-(4,7-biscarboxymethyl(1,4,7)triazacyclonona-1-yl-ethyl)carbonylmethylamino)acetic acid; C463502:(2-(4,7-biscarboxymethyl(1,4,7)triazacyclononan-1-ylethyl)carbonylmethylamino)acetic acid; D000085:Acetates; D002614:Chelating Agents; D006571:Heterocyclic Compounds; D008024:Ligands; D011868:Radioisotopes; D008187:Lutetium; D001729:Bismuth