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Glycoconjugated Re(CO)3+ complexes: syntheses, characterization, cytotoxicity and cellular localization
Bita Abdolahi Sanati1, Ewan L Gilleard1, Tamara Teixeira2
1Department of Chemistry, University of Calgary, Calgary T2N 1N4, Alberta, Canada. faridehj@ucalgary.ca.
Dalton Transactions (Cambridge, England : 2003)
|June 16, 2026
Summary
Rhenium complexes with glycoconjugated ligands show potential as anticancer drugs by targeting glucose transporters (GLUTs). Their cellular uptake and cytotoxicity vary with lipophilicity, suggesting targeted delivery strategies.
Area of Science:
- Inorganic Chemistry
- Medicinal Chemistry
- Cancer Therapeutics
Background:
- Rhenium tricarbonyl complexes are investigated as anticancer agents.
- Enhancing water solubility, biocompatibility, and targeting cancer cells are key challenges.
Purpose of the Study:
- To synthesize and evaluate novel glycoconjugated rhenium(I) complexes for cancer therapy.
- To investigate the role of glucose transporters (GLUTs) in cellular uptake and cytotoxicity.
Main Methods:
- Synthesis of water-stable Re(I) complexes with glycoconjugated diimine ligands.
- Characterization using mass spectrometry, NMR, and X-ray absorption spectroscopy.
- In vitro cytotoxicity assays and cellular distribution studies using X-ray fluorescence microscopy (XFM) and ICP-MS.
Main Results:
- Lipophilic complexes (3 and 4) exhibited moderate cytotoxicity.
- Complex 3 (unprotected sugar) showed greater nuclear accumulation compared to lipophilic complex 4.
- Hydrophilic complex 1 demonstrated significant uptake in HepG2 cells, suggesting GLUT involvement.
Conclusions:
- Glycoconjugated rhenium complexes offer tunable properties for cancer therapy.
- Cellular uptake mechanisms involve both GLUT-mediated transport and passive diffusion.
- Further research into optimizing these complexes for targeted cancer treatment is warranted.
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