Novel hexadentate and pentadentate chelators for 64Cu-based targeted PET imaging

Inseok Sin, Chi Soo Kang, Nilantha Bandara, Xiang Sun, Yongliang Zhong, Buck E. Rogers, Hyun Soon Chong

Research output: Contribution to journalArticle

8 Scopus citations

Abstract

A series of new hexadentate and pentadentate chelators were designed and synthesized as chelators of 64Cu. The new pentadentate and hexadentate chelators contain different types of donor groups and are expected to form neutral complexes with Cu(II). The new chelators were evaluated for complex kinetics and stability with 64Cu. The new chelators instantly bound to 64Cu with high labeling efficiency and maximum specific activity. All 64Cu-radiolabeled complexes in human serum remained intact for 2 days. The 64Cu-radiolabeled complexes were further challenged by EDTA in a 100-fold molar excess. Among the 64Cu- radiolabeled complexes evaluated, 64Cu-complex of the new chelator E was well tolerated with a minimal transfer of 64Cu to EDTA. 64Cu-radiolabeled complex of the new chelator E was further evaluated for biodistribution studies using mice and displayed rapid blood clearance and low organ uptake. 64Cu-chelator E produced a favorable in vitro and in vivo complex stability profiles comparable to 64Cu complex of the known hexadentate NOTA chelator. The in vitro and in vivo data highlight strong potential of the new chelator E for targeted PET imaging application.

Original languageEnglish
Pages (from-to)2553-2562
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number8
DOIs
StatePublished - Apr 15 2014

Keywords

  • Chelating agents
  • NOTA
  • PET imaging

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