New Heteroleptic RuII/Diphosphine Complexes with Cytotoxicity against Human Breast and Murine Ascitic Sarcoma 180 Tumor Cells

Abstract

The preparation, characterization, theoretical calculations and biological application of four Ru II complexes with 2-picolinate (pic), 2,2'-bipyridine (bipy) and P-P as ligands [P-P = 1,1-bis(diphenylphosphino)methane (dppm-1), 1,2-bis(diphenylphosphino)ethane (dppe-2), 1,3-bis(diphenylphosphino)propane (dppp-3) or 1,1'-bis(diphenylphosphino)ferrocene (dppf-4)], is here presented. The complexes 1-4, with general formula [Ru(pic)(P-P)(bipy)]PF 6 , were characterized by elemental analysis and by infrared (IR), UV-Vis, nuclear magnetic resonance (NMR 1 H and 13 P{ 1 H}) spectroscopies, cyclic voltammetry and X-ray crystallography technique. Additionally, preliminary in vitro tests against human breast (MDA-MB-231) and murine ascitic sarcoma 180 (S180) tumor cell lines were carried out, and compared with cisplatin, a reference drug. The drug concentration at which 50% of the cells are viable relative to the control (IC 50) values found for complexes 1, 2, 3 and 4 against MDA-MB-231 tumor cells were around 14.6, 7.6, 3.3 and 0.4 μM, respectively, while against S180 tumor cells these complexes showed IC 50 values of 71.9, 31.3, 11.2 and 3.5 μM, respectively. Therefore, the complexes were more active against MDA-MB-231 than S180.

A Novel Ruthenium(II) Complex With Lapachol Induces G2/M Phase Arrest Through Aurora-B Kinase Down-Regulation and ROS-Mediated Apoptosis in Human Prostate Adenocarcinoma Cells

“…Also, bands around 350 to 600 nm was observed and can be assigned to metal-to-ligands charge transfer (MLCT) and, n → π* transitions of quinone carbonyl groups ( 8 , 39 , 40 ). The cyclic voltammograms showed a process related to Ru II /Ru III oxidation at 1,188 and 1,176 mV, for complex ( 1 ) and ( 2 ), respectively, which are higher than the precursor complexes (0.1–0.6 V) ( 41 ). This observation indicates the higher stability of the complexes after the lapachol coordination to the metal.…”