A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P

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2 Scopus citations

Abstract

The macrocyclic bone-seeking agent, DO2A2P, bears a cyclen core and two pairs of peripheral phosphonate and carboxylate groups. The geometric disposition of the peripheral functionalities gives arise to a pair of geometric isomers: cis-DO2A2P and trans-DO2A2P. In order to compare the biological behavior of the isomer pair, cis-DO2A2P was synthesized. Both isomers were successfully radiolabeled with 177Lu, which might potentiate their applications in both radiotherapy and imaging of bone diseases. Through a set of biological assays including the hydroxyapatite binding, in vitro stability, and in vivo distribution, we demonstrated that the geometric pair of DO2A2P had virtually identical biological properties.

Original languageEnglish (US)
Pages (from-to)571-574
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number3
DOIs
StatePublished - Feb 1 2015

Keywords

  • Bisphosphonate
  • Bone-seeking agent
  • Geometric isomer
  • Lutetium-177
  • Macrocyclics

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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