title: New gold carbene complexes as candidate anticancer agents.
abstract: Three structurally related gold(I) carbene complexes with bulky hydrophobic ligands i.e. 1-3 were investigated in solution for further consideration as candidate anticancer agents. Cytotoxic assays were subsequently conducted on bone marrow-derived preosteoclast cell line of human origin (FLG 29.1) and human colon cancer cells (HCT-116). A far greater cytotoxic activity was measured for compound 1 against HCT-116 cells compared to 2 and 3; conversely, all compounds were highly and similarly active against FLG 29.1 cells. Results obtained for the reaction of complexes 1 and 2 with RNase A documented the occurrence of a weak interaction with this model protein and the formation of a tiny amount of the corresponding adduct. Moreover, a certain reactivity of the complex 2 was also detected toward GSH. The general implications of the obtained results are discussed.
authors: (MetMed) Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy.
authors: Alessandro
authors: A
authors: Pratesi
authors: (MetMed) Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy.
authors: Damiano
authors: D
authors: Cirri
authors: Department of Chemistry, Faculty of Science, University of Kragujevac, R. Domanovića 12, Kragujevac, P. O. Box 60, 34000, Serbia.
authors: Mirjana D
authors: MD
authors: Đurović
authors: Department of Experimental and Clinical Medicine, University of Florence, Viale G.B. Morgagni 50, 50134, Florence, Italy.
authors: Serena
authors: S
authors: Pillozzi
authors: Department of Experimental and Clinical Medicine, University of Florence, Viale G.B. Morgagni 50, 50134, Florence, Italy.
authors: Giulia
authors: G
authors: Petroni
authors: Department of Chemistry, Faculty of Science, University of Kragujevac, R. Domanovića 12, Kragujevac, P. O. Box 60, 34000, Serbia. bugarcic@kg.ac.rs.
authors: Živadin D
authors: ŽD
authors: Bugarčić
authors: (MetMed) Department of Chemistry, University of Florence, Via della Lastruccia 3, 50019, Sesto Fiorentino, Italy. luigi.messori@unifi.it.
authors: Luigi
authors: L
authors: Messori
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D000091344:Filaggrin Proteins; D006046:Gold / Q000737:chemistry* / Q000494:pharmacology*; D045325:HCT116 Cells; D006801:Humans; D008697:Methane / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; C000717249:FLG protein, human; D000091344:Filaggrin Proteins; C030011:carbene; D006046:Gold; D008697:Methane
keywords: Anticancer drugs; ESI–MS; Gold carbene; Protein interaction