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Published on: July 27, 2022
Rhenium(I)-tricarbonyl complexes with methimazole and its selenium analogue: Syntheses, characterization and cell
Farideh Jalilehvand1, Valerie Brunskill1, Tran Si Bui Trung1
1Department of Chemistry, University of Calgary, Calgary, Alberta T2N 1N4, Canada.
New rhenium(I) complexes with thione/selone ligands show significant cytotoxicity against human breast cancer cells. These diimine Re(CO)3+ complexes offer potential as anticancer agents, with stability under UV-A light.
Area of Science:
- Inorganic Chemistry
- Medicinal Chemistry
- Materials Science
Background:
- Rhenium(I) diimine complexes are explored for their photophysical and biological properties.
- Thione and selone ligands can modulate the activity of metal complexes.
- Understanding structure-activity relationships is crucial for developing new therapeutic agents.
Purpose of the Study:
- To synthesize and characterize novel rhenium(I) complexes incorporating thione/selone ligands.
- To evaluate the in vitro cytotoxicity of these complexes against human cancer cell lines.
- To assess the photostability of the complexes under UV-A irradiation.
Main Methods:
- Synthesis of six fac-[Re(CO)3(N,N')X]+ complexes where X = methimazole (MMI) or 1-methylimidazole-2-selone (MSeI).
- Characterization using single-crystal X-ray diffraction, NMR, UV-vis, and vibrational spectroscopy.
- In vitro cytotoxicity assays on MDA-MB-231 (breast cancer) and HEK-293T (embryonic kidney) cell lines.
Main Results:
- All synthesized complexes exhibited significant cytotoxicity against MDA-MB-231 cells, with IC50 values ranging from 8.0 to 55 μM.
- The complex fac-[Re(CO)3(dmphen)(MMI)]+ showed the highest toxicity (IC50 = 8.0 ± 0.2 μM), comparable to a known aqua complex.
- Complexes showed stability upon UV-A light exposure, with no observed carbon monoxide release.
Conclusions:
- Thione/selone ligands can be effectively incorporated into diimine rhenium(I) complexes to impart significant anticancer activity.
- The developed complexes demonstrate promising cytotoxic profiles against human breast cancer cells.
- The photostability suggests potential for applications where light exposure is a factor.
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