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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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ONS-donor ligand based Pt(II) complexes display extremely high anticancer potency through autophagic cell death
Faiz-Ur Rahman1, Amjad Ali2, Hong-Quan Duong3
1Center for Supramolecular Material and Catalysis, Department of Chemistry, Shanghai University, Shanghai, 200444, China; Department of Chemistry, Fudan University, 2005 Songhu Road, Shanghai, 200438, China.
European Journal of Medicinal Chemistry
|January 10, 2019
Summary
New platinum(II) complexes with ONS-donor ligands exhibit potent anticancer activity against lung, colon, and breast cancer cells, outperforming cisplatin. These compounds induce cell death through apoptosis and autophagy, offering a promising alternative cancer therapy.
Area of Science:
- Coordination Chemistry
- Medicinal Chemistry
- Cancer Biology
Background:
- Cisplatin is a widely used platinum-based chemotherapy drug, but its efficacy is limited by resistance and severe side effects.
- There is a continuous need for novel platinum(II) complexes with improved anticancer potency and reduced toxicity.
- ONS-donor ligands offer unique coordination properties that can influence the stability and reactivity of platinum(II) complexes.
Purpose of the Study:
- To synthesize and characterize a novel series of ONS-donor ligand-based platinum(II) complexes.
- To evaluate the in vitro anticancer activity of these complexes against various human cancer cell lines.
- To elucidate the underlying mechanisms of action, including induction of apoptosis, autophagy, and cell cycle arrest.
Main Methods:
- Synthesis of Pt(II)(R-salicylaldimine)Cl and Pt(II)(R-salicylaldimine)(4-picoline)BF4 complexes.
- Characterization using single crystal X-ray analysis, 1H NMR, LCMS, and ESI-MS.
- In vitro anticancer assays on A549, HT-29, and MDA-MB-231 cancer cell lines; assessment of apoptosis, autophagy, cell cycle, DNA interaction, and bacterial growth inhibition.
Main Results:
- The synthesized Pt(II) complexes demonstrated significant anticancer potency against non-small cell lung cancer (A549), colorectal cancer (HT-29), and triple-negative breast cancer (MDA-MB-231) cells.
- These complexes induced poly(ADP-ribose) polymerase (PARP) cleavage, inhibited colony formation, and triggered autophagic cell death via LC3-I/LC3-II expression.
- The complexes also induced p21 expression, activated Caspase3/7-dependent apoptotic signaling, modulated epithelial-mesenchymal-transition (EMT) features, and interacted with plasmid DNA.
Conclusions:
- ONS-donor ligand-based Pt(II) complexes represent a promising new class of anticancer agents with superior efficacy compared to cisplatin.
- These complexes exert their anticancer effects through multiple pathways, including apoptosis, autophagy, and cell cycle arrest.
- Further investigation into these complexes could lead to the development of novel therapeutic strategies for various cancers.
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