Copper complexes are coming out as metal-based drugs candidates for the treatment of cancer, due to their wide structural variability, biologically accessible redox properties and bioavailability. Recently, in our quest to find suitable ligands in the design of copper-based anticancer agents, we focused our attention on the synthesis of copper complexes of bis(azol-1-yl)carboxylate ligands functionalized with biomolecules. In addition, Cu(II) complexes of alkyl bis(pyrazol-1-yl)acetate ligands have been investigated for the development of a new and more efficient promoter for the Kharasch-Sosnovsky reaction to oxidize alkenes in allyl position. Since such coordination compounds have low solubility in aqueous medium, it is necessary to design a strategic approach allowing for drug delivery. By conjugating the copper complexes with hydrophilic gold nanoparticles, it is possible to improve their solubility and stability in water, increasing their bioavailability. Moreover, these drug delivery systems allow the investigation of a slow and controlled release of copper complexes. In this context, we carried out a spectroscopic investigation of the molecular, electronic structure and coordination geometry of a selection of Cu(II)-coordination compounds, by means of complementary X-ray techniques induced by Synchrotron Radiation: the molecular and electronic structure were probed by means of SR-XPS and NEXAFS, the oxidation state and the local coordination chemistry of the metal ion were assessed by Cu K-edge XAFS analysed in the near edge (XANES) and extended (EXAFS) regions.
Study of the Molecular and Electronic Structure of Copper Coordination Compounds Conjugated to Gold Nanoparticles as Innovative Anticancer Drugs
Maura Pellei;Carlo Santini;Luca Bagnarelli;
2019-01-01
Abstract
Copper complexes are coming out as metal-based drugs candidates for the treatment of cancer, due to their wide structural variability, biologically accessible redox properties and bioavailability. Recently, in our quest to find suitable ligands in the design of copper-based anticancer agents, we focused our attention on the synthesis of copper complexes of bis(azol-1-yl)carboxylate ligands functionalized with biomolecules. In addition, Cu(II) complexes of alkyl bis(pyrazol-1-yl)acetate ligands have been investigated for the development of a new and more efficient promoter for the Kharasch-Sosnovsky reaction to oxidize alkenes in allyl position. Since such coordination compounds have low solubility in aqueous medium, it is necessary to design a strategic approach allowing for drug delivery. By conjugating the copper complexes with hydrophilic gold nanoparticles, it is possible to improve their solubility and stability in water, increasing their bioavailability. Moreover, these drug delivery systems allow the investigation of a slow and controlled release of copper complexes. In this context, we carried out a spectroscopic investigation of the molecular, electronic structure and coordination geometry of a selection of Cu(II)-coordination compounds, by means of complementary X-ray techniques induced by Synchrotron Radiation: the molecular and electronic structure were probed by means of SR-XPS and NEXAFS, the oxidation state and the local coordination chemistry of the metal ion were assessed by Cu K-edge XAFS analysed in the near edge (XANES) and extended (EXAFS) regions.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.