Ruthenium arene complexes are getting more and more interesting, especially in medicinal chemistry as valid anticancer compounds. Ru(II)-arene complexes with β-ketoamine ligands derived from 4-acyl-5-pyrazolones possess significant anticancer activity in vitro, moreover it was found that minor changes to the β-ketoamine ligand lead to considerable changes in cytotoxicity. As continuation of a previous work fulfilled by our research group, a series of novel Ruthenium arene derivatives containing β-ketoamine ligands (HL' in general) has been synthetized and characterized by spectroscopy, elemental analysis and single-crystal X-ray diffraction. Spectroscopic and crystallographic data showed that the ligands in their anionic form coordinate to ruthenium ion in a chelating κ2 N,O-bidentate mode, affording 1:1 derivatives with formula [(arene)Ru(L')Cl]. Finally the anticancer activity of the ligands and the complexes has been tested in vitro against the human ovarian carcinoma cell line A2780 and its cisplatin-resistant equivalent A2780R.
New Ruthenium(II) Arene Complexes with N,O-Chelating Ketoamine Ligands: Synthesis, Structure and Biological Activity
PETRINI, Agnese;CONDELLO, FRANCESCA;ORBISAGLIA, SERENA;PALMUCCI, JESSICA;MARCHETTI, Fabio;PETTINARI, Riccardo;PETTINARI, Claudio;
2014-01-01
Abstract
Ruthenium arene complexes are getting more and more interesting, especially in medicinal chemistry as valid anticancer compounds. Ru(II)-arene complexes with β-ketoamine ligands derived from 4-acyl-5-pyrazolones possess significant anticancer activity in vitro, moreover it was found that minor changes to the β-ketoamine ligand lead to considerable changes in cytotoxicity. As continuation of a previous work fulfilled by our research group, a series of novel Ruthenium arene derivatives containing β-ketoamine ligands (HL' in general) has been synthetized and characterized by spectroscopy, elemental analysis and single-crystal X-ray diffraction. Spectroscopic and crystallographic data showed that the ligands in their anionic form coordinate to ruthenium ion in a chelating κ2 N,O-bidentate mode, affording 1:1 derivatives with formula [(arene)Ru(L')Cl]. Finally the anticancer activity of the ligands and the complexes has been tested in vitro against the human ovarian carcinoma cell line A2780 and its cisplatin-resistant equivalent A2780R.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
