Literature DB >> 18313802

Bisphosphonate sequestering agents. Synthesis and preliminary evaluation for in vitro and in vivo uranium(VI) chelation.

Marcin Sawicki1, Delphine Lecerclé, Gérard Grillon, Béatrice Le Gall, Anne-Laure Sérandour, Jean-Luc Poncy, Théodorine Bailly, Ramon Burgada, Marc Lecouvey, Vincent Challeix, Antoine Leydier, Stephane Pellet-Rostaing, Eric Ansoborlo, Frédéric Taran.   

Abstract

A library of bisphosphonate-based ligands was prepared using solution-phase parallel synthesis and tested for its uranium-binding properties. With the help of a screening method, based on a chromophoric complex displacement procedure, 23 dipodal and tripodal chelates bearing bisphosphonate chelating functions were found to display very high affinity for the uranyl ion and were selected for evaluation of their in vivo uranyl-removal efficacy. Among them, 11 ligands induced a huge modification of the uranyl biodistribution by deviating the metal from kidney and bones to liver. Among the other ligands, the most potent was the dipodal bisphosphonate 3C which reduced the retention of uranyl and increased its excretion by around 10% of the injected metal.

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Year:  2008        PMID: 18313802     DOI: 10.1016/j.ejmech.2008.01.018

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Stable Chelation of the Uranyl Ion by Acyclic Hexadentate Ligands: Potential Applications for 230U Targeted α-Therapy.

Authors:  Joshua J Woods; Ryan Unnerstall; Abbie Hasson; Diane S Abou; Valery Radchenko; Daniel L J Thorek; Justin J Wilson
Journal:  Inorg Chem       Date:  2022-02-09       Impact factor: 5.436

2.  Click and Cut: a click chemistry approach to developing oxidative DNA damaging agents.

Authors:  Natasha McStay; Creina Slator; Vandana Singh; Alex Gibney; Fredrik Westerlund; Andrew Kellett
Journal:  Nucleic Acids Res       Date:  2021-10-11       Impact factor: 16.971

  2 in total

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