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 da...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-06, Vol.18 (11), p.3436-3439
Main Authors: Chong, Hyun-Soon, Song, Hyun A., Birch, Noah, Le, Thien, Lim, Sooyoun, Ma, Xiang
Format: Article
Language:English
Subjects:
177Lu
212Bi
213Bi
Acetates - chemical synthesis
Acetates - chemistry
Acetates - pharmacology
Biological and medical sciences
Bismuth
Chelating Agents - chemical synthesis
Chelating Agents - chemistry
Chelating Agents - pharmacology
Contrast media. Radiopharmaceuticals
Crystallography, X-Ray
Drug Design
Heterocyclic Compounds - chemical synthesis
Heterocyclic Compounds - chemistry
Heterocyclic Compounds - pharmacology
Kinetics
Ligands
Lutetium
Medical sciences
Metal binding ligand
Molecular Conformation
Molecular Structure
NETA
Pharmacology. Drug treatments
Radioimmunotherapy
Radioisotopes
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Summary: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 212Bi, 213Bi, and 177Lu.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.03.084