Anticancer Compounds

Anticancer Compounds

In medicinal inorganic chemistry, copper-coordinated compounds are largely studied for the fact that copper, being an endogenous metal, result less toxic than others well-known anticancer compounds as cis-platin.  In these papers, different copper-coordinated complexes have been synthesized and thei anticancer properties have been evaluated. Furthermore, their  mechanism of action inside cells have been largely studied.













  • Barilli A., Atzeri C., Bassanetti I., Ingoglia F., Dall’Asta V., Bussolati O., Maffini M., Mucchino C., and Marchiò L. “Oxidative Stress Induced by Copper and Iron Complexes with 8-Hydroxyquinoline Derivatives Causes Paraptotic Death of HeLa Cancer Cells”. Mol. Pharmaceutics, 2014, 11 (4), 1151–1163


  • Tardito S., Barilli A., Bassanetti I., Tegoni M., Bussolati O., Franchi-Gazzola R., Mucchino C,, Marchiò L.. “Copper-Dependent Cytotoxicity of 8-Hydroxyquinoline derivatives correlates with their hydrophobicity and does not require caspase activation.”, J.Med.Chem., 2012, 55(23), 10448-10459.


  • Tardito S., Bassanetti I., Bignardi C., Elviri L., Tegoni M., Mucchino C., Bussolati O., Franchi-Gazzola R., Marchiò L. “Copper binding agents acting as copper ionophores lead to caspase inhibition and paraptotic cell death in human cancer cells.”, JACS , 2011, 133, 6235-6242.






  • Copper Binding Agents Acting as Copper Ionophores Lead to Caspase Inhibition and Paraptotic Cell Death in Human Cancer CellsSaverio Tardito, Irene Bassanetti, Chiara Bignardi, Lisa Elviri, Matteo Tegoni, Claudio Mucchino, Ovidio Bussolati, Renata Franchi-Gazzola, and Luciano Marchio.We report a quantitative structure activity relationship study of a new class of pyrazole-pyridine copper complexes that establishes a clear correlation between the ability to promote copper accumulation and cytotoxicity. Intracellular metal accumulation is maximized when ligand lipophilicity allows the complex to rapidly cross the membrane.J. Am. Chem. Soc. 2011, 133, 6235–6242
  • Copper-Dependent Cytotoxicity of 8‑Hydroxyquinoline Derivatives Correlates with Their Hydrophobicity and Does Not Require Caspase ActivationSaverio Tardito, Amelia Barilli, Irene Bassanetti, Matteo Tegoni, Ovidio Bussolati, Renata Franchi-Gazzola, Claudio Mucchino, and Luciano Marchio.This study reports the structure− activity relationship of a series of 8-hydroxoquinoline derivatives (8-HQs) and focuses on the cytotoxic activity of 5-Cl-7-I-8-HQ (clioquinol, CQ) copper complex (Cu(CQ)). 8-HQs alone cause a dose-dependent loss of viability of the human tumor HeLa and PC3 cells, but the coadministration of copper increases the ligands eff ects, with extensive cell death occurring in both cell lines.J. Med. Chem. 2012, 55, 10448−10459
  • Oxidative Stress Induced by Copper and Iron Complexes with 8‑Hydroxyquinoline Derivatives Causes Paraptotic Death of HeLa Cancer CellsAmelia Barilli, Corrado Atzeri, Irene Bassanetti, Filippo Ingoglia, Valeria Dall’Asta, Ovidio Bussolati, Monica Maffini, Claudio Mucchino, and Luciano Marchio.Here, we report the antiproliferative/cytotoxic properties of 8-hydroxyquinoline (8-HQ) derivatives on HeLa cells in the presence of transition metal ions (Cu2+ , Fe3+ , Co2+ ,Ni2+ ). Two series of ligands were tested, the arylvinylquinolinic L1−L8  and the arylethylenequinolinic L9−L16 , which can all interact with metal ions by virtue of the N,O donor set of 8-HQ.Mol. Pharmaceutics 2014, 11, 1151−1163