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Updated: Jul 6, 2025

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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
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Anticancer Study on IrIII and RhIII Half-Sandwich Complexes with the Bipyridylsulfonamide Ligand
Mateusz Kowalik1, Joanna Masternak2, Mateusz Olszewski3
1Faculty of Chemistry, University of Gdańsk, Wita Stwosza 63, 80-308 Gdańsk, Poland.
Inorganic Chemistry
|January 4, 2024
Summary
New iridium and rhodium complexes with a sulfonamide ligand were synthesized. The rhodium complex and ligand show potential for pharmaceutical development by inducing cancer cell death via a caspase-dependent pathway.
Area of Science:
- Organometallic Chemistry
- Medicinal Chemistry
- Biochemistry
Background:
- Organometallic half-sandwich complexes of iridium(III) and rhodium(III) were synthesized using a novel sulfonamide ligand.
- The structural characterization and coordination chemistry of these complexes were investigated.
Purpose of the Study:
- To explore the biological interactions of the synthesized sulfonamide ligand (L) and its iridium(III) (1) and rhodium(III) (2) complexes.
- To evaluate the potential therapeutic applications of these compounds.
Main Methods:
- Synthesis and crystal structure analysis of ligand (L) and complexes (1, 2).
- Spectroscopic techniques (e.g., NMR, IR, Mass Spectrometry) for characterization.
- In vitro studies involving carbonic anhydrase (CA), human serum albumin (HSA), CT-DNA, cancer cell lines, and non-malignant cells.
Main Results:
- Complex (1) showed no antiproliferative activity due to high glutathione (GSH) binding affinity.
- Ligand (L) exhibited competitive inhibition of CA, while complexes (1, 2) showed uncompetitive inhibition.
- All compounds interacted with HSA, altering its secondary structure, and compounds (L, 2) induced caspase-dependent cell death.
Conclusions:
- The sulfonamide ligand (L) and rhodium(III) complex (2) demonstrate promising cytotoxic effects.
- These compounds represent potential lead structures for further pharmaceutical and therapeutic research.

