期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 3, 页码 763-770出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm8012135
关键词
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资金
- DFG-Deutsche Forschungsgemeinschaft [FOR-630]
- BMBF-Bundesministerium fur Bildung and Forschung [CHN 08/007]
- Portuguese Foundation for Science and Technology [SFRH/BD/27262/2006]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/27262/2006] Funding Source: FCT
The novel luminescent gold(I) complex [(N-N',N'-dimethylaminoethyl)-1,8-naphthalimide-4-sulfide](triethylphosphine)gold(I) was prepared and investigated for its primary biological properties. Cell culture experiments revealed strong antiproliferative effects and induction of apoptosis via mitochondrial pathways. Biodistribution studies by fluorescence microscopy and atomic absorption spectroscopy showed the uptake into cell organelles, all accumulation in the nuclei of tumor cells, and a homogeneous distribution in zebrafish embryos. In vivo monitoring of vascularisation in developing zebrafish embryos revealed a significant anti-angiogenic potency of the complex. Mechanistic experiments indicated that the inhibition of thioredoxin reductase (based on the covalent binding of a gold triethylphosphine fragment) might be involved in the pharmacodynamic behavior of this novel gold species.
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