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

[Display omitted] 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 t...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (3), p.571-574
Hauptverfasser: Hao, Guiyang, Liu, Wei, Hassan, Gedaa, Öz, Orhan K., Kovacs, Zoltan, Sun, Xiankai
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Sprache:eng
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Zusammenfassung:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.12.016