Copper complexes with phosphonium containing hydrazone ligand: topoisomerase inhibition and cytotoxicity study
| Autor: | Sze Koon Lee, Kong Mun Lo, Shin Thung Chew, Kae Shin Sim, Wuen Yew Teoh, Mok Piew Heng, Kong Wai Tan |
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| Rok vydání: | 2013 |
| Předmět: |
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Molecular Magnetic Resonance Spectroscopy Spectrophotometry Infrared Stereochemistry chemistry.chemical_element Hydrazone Topoisomerase-I Inhibitor Crystallography X-Ray Ligands chemistry.chemical_compound Deprotonation Cell Line Tumor Drug Discovery Humans Phosphonium Cytotoxicity Pharmacology chemistry.chemical_classification biology Topoisomerase Organic Chemistry Hydrazones Phosphorus General Medicine Copper Enzyme chemistry biology.protein Drug Screening Assays Antitumor Topoisomerase I Inhibitors |
| Zdroj: | European journal of medicinal chemistry. 76 |
| ISSN: | 1768-3254 |
| Popis: | Four new copper(II) complexes containing phosphonium substituted hydrazone (L) with the formulations [CuL]Cl( 3 ), [Cu(phen)L]Cl( 4 ), [Cu(bpy)L]Cl( 5 ), [Cu(dbpy)L]Cl( 6 ), (where L = doubly deprotonated hydrazone; phen = 1,10′-phenanthroline; bpy = 2,2′-bipyridine; dbpy = 5,5′-dimethyl-2,2′-bipyridine) have been synthesized. The compounds were characterized by elemental analysis, spectroscopic methods and in the case of crystalline products by X-ray crystallography. The cytotoxicity and topoisomerase I (topo I) inhibition activities of these compounds were studied. It is noteworthy that the addition of N,N-ligands to the copper(II) complex lead to the enhancement in the cytotoxicity of the compounds, especially against human prostate adenocarcinoma cell line (PC-3). Complex 4 exhibits the highest activity against PC-3 with the IC 50 value of 3.2 μΜ. The complexes can also inhibit topo I through the binding to DNA and the enzyme. |
| Databáze: | OpenAIRE |
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