Efficient synthesis and evaluation of bimodal ligand NETA

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3436-9. doi: 10.1016/j.bmcl.2008.03.084. Epub 2008 Apr 8.

Abstract

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Acetates / chemical synthesis*
  • Acetates / chemistry
  • Acetates / pharmacology*
  • Bismuth
  • Chelating Agents / chemical synthesis*
  • Chelating Agents / chemistry
  • Chelating Agents / pharmacology
  • Crystallography, X-Ray
  • Drug Design
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology*
  • Kinetics
  • Ligands
  • Lutetium
  • Molecular Conformation
  • Molecular Structure
  • Radioimmunotherapy
  • Radioisotopes*

Substances

  • (2-(4,7-biscarboxymethyl(1,4,7)triazacyclonona-1-yl-ethyl)carbonylmethylamino)acetic acid
  • (2-(4,7-biscarboxymethyl(1,4,7)triazacyclononan-1-ylethyl)carbonylmethylamino)acetic acid
  • Acetates
  • Chelating Agents
  • Heterocyclic Compounds
  • Ligands
  • Radioisotopes
  • Lutetium
  • Bismuth