Study of the effect of the chromophore and nuclearity on the aggregation and potential biological activity of gold(I) alkynyl complexes

被引:29
作者
Gavara, Raquel [1 ]
Aguilo, Elisabet [1 ]
Schur, Julia [2 ]
Llorca, Jordi [3 ,4 ]
Ott, Ingo [2 ]
Rodriguez, Laura [1 ]
机构
[1] Univ Barcelona, Dept Quim Inorgan, Marti & Franques 1-11, Barcelona 08028, Spain
[2] Tech Univ Carolo Wilhelmina Braunschweig, Inst Med & Pharmaceut Chem, Beethovenstr 55, D-38106 Braunschweig, Germany
[3] Univ Politecn Cataluna, Inst Tecn Energet, Diagonal 647, E-08028 Barcelona, Spain
[4] Univ Politecn Cataluna, Ctr Recerca NanoEngn, Diagonal 647, E-08028 Barcelona, Spain
关键词
Gold; Alkynyl; Thioredoxin reductase; Cytotoxicity; Luminescence; ANTITUMOR-ACTIVITY; CARBENE COMPLEXES; IN-VITRO; CYTOTOXICITY; DERIVATIVES; INHIBITION; MECHANISMS; DRUGS;
D O I
10.1016/j.ica.2016.03.012
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The synthesis and characterization of four organometallic gold(I) complexes containing different water soluble phosphanes (TPPTS, PTA and DAPTA) and chromophoric units (4-pyridylethynyl and propargyloxycoumarin) is here reported. The analysis of their absorption and emission spectra led us to attribute their luminescent behavior to the chromophoric organic ligands. Moreover, the presence of the gold(I) metal atom has been observed to be the responsible of an efficient intersystem crossing process responsible for the observed phosphorescence emission. Broad emission bands are observed in most cases due to the formation of organized aggregates in solution in agreement with microscopic characterization. Biological activity of the complexes showed very low effects against tumor cell growth but an inhibitory potency against thioredoxin reductase (TrxR). The missing/low cytotoxic effects could be related to a low bioavailability as determined by atomic absorption spectroscopy. (C) 2016 Elsevier B.V. All rights reserved.
引用
收藏
页码:189 / 197
页数:9
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