Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Preparation of an Amino Acid Based DTPA as a BFCA for Radioimmunotherapy

  • Choi, Kang-hyuk (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute) ;
  • Hong, Young-Don (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute) ;
  • Pyun, Mi-Sun (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute) ;
  • Choi, Sun-Ju (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute)
  • Published : 2006.08.20
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Abstract

For the purpose of developing more effective chelating agents, we have synthesized a diethylene triamine pentaacetic acid(DTPA) analogue by using an amino acid. S-(N-Boc-aminophenyl)-Cys(t-Bu4-DTPA) methylester was prepared in 6 steps with total yield of 47.9%. For the sake of introducing a biomolecule to the DTPA derivative, a selective hydrolysis was performed with 3 M HCl/Ethylacetate = 1 : 3 ($25{^{\circ}C}$, 30 min, vigorous stirring). $^{166}Ho$-Cys-DTPA and $^{166}Ho$-Biotin-Cys-DTPA were prepared by mixing $^{166}Ho$ with DTPA derivatives at room temp in a HCl solution (pH = 5) and the radiochemical stabilities (> 99%) were maintained for over 6 hrs in vitro.

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