Antiproliferative Activities of Diimine-Based Mixed Ligand Copper(II) Complexes

• DOI: 10.1021/acscombsci.9b00202
• Publication Date: 2020-01-08T15:22:35Z
• Authors: Nazanin Kordestani; Hadi Amiri Rudbari; Alexandra R. Fern...; Luís R. Raposo; Pedro V. Baptista; Daniela Ferreira; Giuseppe Bruno; Giovanni Bella; Rosario Scopelliti; Jason D. Braun; David E. Herbert; Olivier Blacque
• Keywords: Diimine; IC50; Viability assay

A series of Cu(diimine)(X-sal)(NO3) complexes, where the diimine is either 2,2′-bipyridine (bpy) or 1,10-phenanthroline (phen) and X-sal a monoanionic halogenated salicylaldehyde (X = Cl, Br, I, H), have been synthesized characterized by elemental analysis X-ray crystallography. Penta-coordinate geometries copper(II) were observed for all cases. The influence coligands different halogen atoms on antiproliferative activities toward human cancer cell lines investigated. All Cu(II) complexes able to induce loss A2780 ovarian carcinoma viability, with phen derivatives more active than bpy derivatives. In contrast, no in vitro effects against HCT116 colorectal line. These cytotoxicity differences not due intracellular concentration determined inductively coupled plasma atomic emission spectroscopy. small effect substituents phenolic ring was observed, X Cl being most highly cells among derivatives, while Br presented lowest IC50 analogs. Importantly, reduction normal primary fibroblasts viability presence (IC50 > 40 μM). Mechanistically, complex 1 seems stronger apoptotic response higher increase mitochondrial membrane depolarization an increased level reactive oxygen species (ROS) compared 3. Together, these data low cisplatin line demonstrate potential further vivo studies.