title: Synthesis and biological assays on cancer cells of dinuclear gold complexes with novel functionalised di(N-heterocyclic carbene) ligands.
abstract: New dinuclear di(N-heterocyclic carbene) silver(I), gold(I) and gold(III) complexes have been synthesised and their antiproliferative effects towards various cancer cell lines have been screened. The di(N-heterocyclic carbene) ligands have a propylene linker between the carbene moieties and the imidazole backbone has been functionalised with a 1-benzyl- or 1-PEG-1,2,3-triazole ring (PEG=poly(ethylene glycol)) via a CuAAC (copper azido alkyne cycloaddition) reaction. The resulting gold(I) and gold(III) complexes display an antiproliferative activity superior to that of the unfunctionalised pristine complexes together with a higher selectivity towards cancerous cells with respect to healthy cells.
authors.affiliation: Dipartimento di Scienze Chimiche, Università degli Studi di Padova, via F. Marzolo 1, 35131 Padova, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Baron
authors.affiliation: Institut de Physique et Chimie des Matériaux de Strasbourg (IPCMS), CNRS-Université de Strasbourg UMR7504, 23 rue du Loess BP 43, 67034 Strasbourg, France; University of Strasbourg, Institute for Advanced Study (USIAS), 5 allée du Général Rouvillois, 67083 Strasbourg, France. Electronic address: bellemin@unistra.fr.
authors.forename: Stéphane
authors.initials: S
authors.lastname: Bellemin-Laponnaz
authors.affiliation: Dipartimento di Scienze Chimiche, Università degli Studi di Padova, via F. Marzolo 1, 35131 Padova, Italy. Electronic address: cristina.tubaro@unipd.it.
authors.forename: Cristina
authors.initials: C
authors.lastname: Tubaro
authors.affiliation: Dipartimento di Scienze Chimiche, Università degli Studi di Padova, via F. Marzolo 1, 35131 Padova, Italy.
authors.forename: Marino
authors.initials: M
authors.lastname: Basato
authors.affiliation: Dipartimento di Scienze Chimiche, Università degli Studi di Padova, via F. Marzolo 1, 35131 Padova, Italy.
authors.forename: Sara
authors.initials: S
authors.lastname: Bogialli
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi di Padova, via F. Marzolo 5, 35131 Padova, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Dolmella
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000494:pharmacology; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D003300:Copper / Q000737:chemistry; D061565:Cycloaddition Reaction; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008024:Ligands; D008697:Methane / Q000031:analogs & derivatives* / Q000737:chemistry; D009928:Organ Specificity; D050607:Organogold Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry; D012834:Silver / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D007093:Imidazoles; D008024:Ligands; D050607:Organogold Compounds; C030011:carbene; D012834:Silver; D011092:Polyethylene Glycols; D003300:Copper; D008697:Methane; D002945:Cisplatin
keywords: Antiproliferative effects; CuAAC; Dinuclear complexes; Gold complexes; Metallopharmaceuticals; N-heterocyclic dicarbenes