Library of second-generation cycloruthenated compounds and evaluation of their biological properties as potential anticancer drugs: Passing the nanomolar barrier

被引:78
作者
Fetzer, Ludivine [1 ]
Boff, Bastien [1 ]
Ali, Moussa [1 ]
Meng Xiangjun [2 ]
Collin, Jean-Paul [1 ]
Sirlin, Claude [1 ]
Gaiddon, Christian [2 ]
Pfeffer, Michel [1 ]
机构
[1] Univ Strasbourg, CNRS, UMR 7177, Inst Chim, F-67000 Strasbourg, France
[2] Univ Strasbourg, INSERM, UMRS 692, F-67000 Strasbourg, France
关键词
CYCLOMETALATED RUTHENIUM(II) COMPLEXES; GLUCOSE-OXIDASE; LIQUID-CHROMATOGRAPHY; CRYSTAL-STRUCTURES; ELECTRON-TRANSFER; CANCER-CELLS; LIGANDS; PHEN; ELECTROCHEMISTRY; HYDROPHOBICITY;
D O I
10.1039/c1dt10322a
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
A library of 32 organoruthenium compounds has been synthesised. Known and novel C-N cyclometalated compounds as well as N-C-N and N-N-C pincer derivatives of this metal have been used in this purpose. Most of the compounds have been tested for their in vitro antitumoral behaviours, good to excellent activities have thus been found. Several of the newly synthesized compounds pass the symbolic barrier of the nanomolar range for their IC50 indicating a critical improvement. The level of activity is tentatively correlated to physicochemical properties of the compounds such as their Ru-III/II redox potential and their lipophilicity (log P).
引用
收藏
页码:8869 / 8878
页数:10
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