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

Research output: Contribution to journalArticle

2 Citations (Scopus)

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

Fingerprint

Isomers
Bone
Bone and Bones
Organophosphonates
Bone Diseases
Durapatite
Biological Assay
Radiotherapy
Assays
Imaging techniques
cis-DO2A2P
trans-DO2A2P
cyclen
In Vitro Techniques

Keywords

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

ASJC Scopus subject areas

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

Cite this

A comparative study of trans- and cis-isomers of a bone-seeking agent, DO2A2P. / Hao, Guiyang; Liu, Wei; Hassan, Gedaa; Öz, Orhan K.; Kovacs, Zoltan; Sun, Xiankai.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 25, No. 3, 01.02.2015, p. 571-574.

Research output: Contribution to journalArticle

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AU - Liu, Wei

AU - Hassan, Gedaa

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AU - Kovacs, Zoltan

AU - Sun, Xiankai

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