Literature DB >> 25541387

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

Guiyang Hao1, Wei Liu2, Gedaa Hassan1, Orhan K Öz1, Zoltan Kovacs3, Xiankai Sun4.   

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 (177)Lu, 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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Bisphosphonate; Bone-seeking agent; Geometric isomer; Lutetium-177; Macrocyclics

Mesh：

Substances：

Year:  2014        PMID： 25541387      PMCID： PMC4386885          DOI： 10.1016/j.bmcl.2014.12.016

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  11 in total

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