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Related Experiment Videos

Rhodium-105 tetrathioether complexes: radiochemistry and initial biological evaluation.

N Goswami1, C Higginbotham, W Volkert

  • 1Department of Chemistry, University of Missouri, Columbia 65211, USA.

Nuclear Medicine and Biology
|March 9, 2000
PubMed
Summary

New rhodium(III) complexes with carboxylic acid groups were synthesized. The cis-[Rh(III)Cl2(2,5,8,11-tetrathiadodecane-1,12-dicarboxylic acid)]+ complex demonstrated promising in vivo characteristics for radiopharmaceutical development.

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Area of Science:

  • Inorganic Chemistry
  • Radiopharmaceutical Chemistry
  • Medicinal Chemistry

Background:

  • Rhodium(III) complexes are explored for therapeutic applications.
  • Tetrathioether ligands offer unique coordination properties.
  • Carboxylic acid groups can influence pharmacokinetic profiles.

Purpose of the Study:

  • Synthesize and characterize novel rhodium(III) complexes with acyclic tetrathioether ligands bearing carboxylic acid groups.
  • Evaluate the stability of these complexes under physiological conditions.
  • Assess the in vivo behavior and identify promising candidates for radiopharmaceutical development.

Main Methods:

  • Synthesis of three distinct rhodium(III) tetrathioether complexes.
  • Characterization using spectroscopic and analytical techniques.

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  • In vitro stability assays under physiological conditions.
  • In vivo studies in normal mice to determine clearance pathways and biodistribution.

    • Main Results:

    • Successful synthesis and characterization of rhodium(III) complexes.
    • Demonstrated stability under physiological conditions for promising candidates.
    • Renal/urinary system identified as the primary clearance route, correlating with carboxylate groups.
    • The cis-[Rh(III)Cl2(2,5,8,11-tetrathiadodecane-1,12-dicarboxylic acid)]+ complex exhibited favorable in vivo characteristics.

    Conclusions:

    • The synthesized rhodium(III) complexes show potential as therapeutic agents.
    • The presence of pendant carboxylate groups facilitates renal clearance.
    • The cis-[Rh(III)Cl2(2,5,8,11-tetrathiadodecane-1,12-dicarboxylic acid)]+ complex is a strong candidate for further development as a radiopharmaceutical.