Synthesis and Antiproliferative Activity of New Ruthenium Complexes with Ethacrynic-Acid-Modified Pyridine and Triphenylphosphine Ligands

被引：61

作者：

Agonigi, Gabriele ^{[1
]}

Riedel, Tina ^{[2
]}

Zacchini, Stefano ^{[3
]}

Paunescu, Emilia ^{[2
]}

Pampaloni, Guido ^{[1
]}

Bartalucci, Niccolo ^{[1
]}

Dyson, Paul J. ^{[2
]}

Marchetti, Fabio ^{[1
]}

机构：

[1] Univ Pisa, Dipartimento Chim & Chim Ind, I-56124 Pisa, Italy

[2] Ecole Polytech Fed Lausanne, Inst Sci & Ingn Chim, CH-1015 Lausanne, Switzerland

[3] Univ Bologna, Dipartimento Chim Ind Toso Montanari, I-40136 Bologna, Italy

来源：

INORGANIC CHEMISTRY | 2015年 / 54卷 / 13期

基金：

瑞士国家科学基金会;

关键词：

ARENE ANTICANCER COMPLEXES; RUTHENIUM(II)-ARENE COMPLEXES; CONDUCTIVITY MEASUREMENTS; TRANSFERASE P1-1; RATIONAL DESIGN; IN-VITRO; PHASE-I; DRUG; COORDINATION; CANCER;

D O I：

10.1021/acs.inorgchem.5b00802

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Pyridine- and phosphine-based ligands modified with ethacrynic acid (a broad acting glutathione transferase inhibitor) were prepared and coordinated to ruthenium(II)-arene complexes and to a ruthenium(III) NAMI-A type complex. All the compounds (ligands and complexes) were fully characterized by analytical and spectroscopic methods and, in one case, by single-crystal Xray diffraction. The in vitro anticancer activity of the compounds was studied, with the compounds displaying moderate cytotoxicity toward the human ovarian cancer cell lines. All the complexes led to similar levels of residual GST activity in the different cell lines, irrespective of the stability of the Ru-ligand bond.

引用

页码：6504 / 6512

页数：9

共 57 条

[1] [Ru(η6-p-cymene)Cl2(pta)] (pta=1,3,5-triaza-7-phosphatricyclo[3.3.1.1]decane):: a water soluble compound that exhibits pH dependent DNA binding providing selectivity for diseased cells [J].