Gold(I) thiotetrazolates as thioredoxin reductase inhibitors and antiproliferative agents

被引：45

作者：

Serebryanskaya, Tatiyana V. ^{[1
,2
,3
]}

Lyakhov, Alexander S. ^{[2
]}

Ivashkevich, Ludmila S. ^{[2
]}

Schur, Julia ^{[1
]}

Frias, Corazon ^{[4
]}

Prokop, Aram ^{[4
]}

Ott, Ingo ^{[1
]}

机构：

[1] Tech Univ Carolo Wilhelmina Braunschweig, Inst Med & Pharmaceut Chem, D-38106 Braunschweig, Germany

[2] Belarusian State Univ, Phys Chem Problems Res Inst, Minsk 220030, BELARUS

[3] St Petersburg State Univ, Inst Chem, St Petersburg 198504, Russia

[4] Childrens Hosp Cologne, Dept Paediat Oncol, D-50735 Cologne, Germany

来源：

DALTON TRANSACTIONS | 2015年 / 44卷 / 03期

关键词：

TRANSITION-METAL-COMPLEXES; IN-VITRO CYTOTOXICITY; CELLULAR UPTAKE; PLATINUM(II); DIPHOSPHINE; LIGANDS; GROWTH; CELLS;

D O I：

10.1039/c4dt03105a

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Gold(I) complexes with phosphane and thiotetrazolate ligands were prepared and investigated as a new type of bioactive gold metallodrugs. The complexes triggered very efficient inhibition of the enzyme thioredoxin reductase (TrxR), which is an important molecular target for gold species. Strong cytotoxic effects were observed in MDA-MB-231 breast adenocarcinoma and HT-29 colon carcinoma cells, and the complexes also caused strong effects in vincristine resistant Nalm-6 leukemia cells. Cellular uptake studies showed elevated cellular gold levels for complexes containing a triphenylphosphane ligand, whereas trifurylphosphane analogues accumulated at significantly lower cellular concentrations.

引用

页码：1161 / 1169

页数：9

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