含氮杂环卡宾配体的金（I）配合物的合成、结构及其对癌细胞的选择性毒性
Synthesis, structures, and selective toxicity to cancer cells of gold(I) complexes involving N-heterocyclic carbene ligands.
作者信息
Boselli Luca, Ader Isabelle, Carraz Maëlle, Hemmert Catherine, Cuvillier Olivier, Gornitzka Heinz
机构信息
CNRS, LCC (Laboratoire de Chimie de Coordination), 205 route de Narbonne, BP 44099, F-31077 Toulouse cedex 4, France; Université de Toulouse, UPS, INP, LCC, F-31077 Toulouse, France.
CNRS, Institut de Pharmacologie et de Biologie Structurale, Toulouse, France; Université de Toulouse, UPS, IPBS, Toulouse, France.
出版信息
Eur J Med Chem. 2014 Oct 6;85:87-94. doi: 10.1016/j.ejmech.2014.07.086. Epub 2014 Jul 24.
New gold(I) complexes containing two 1-[2-(diethylamino)ethyl]imidazolydene ligands have been synthesized and characterized. The X-ray structures of two key compounds are presented. All complexes have been tested for their antiproliferative activities in prostate cancer cell line PC-3. Lipophilicity (Log P) has been determined for these complexes. The most active complex has been tested for the cytotoxic activities in five human cancer cell lines and primary endothelial cells. The most active complex demonstrated a potent selectivity for cancer cells.
已合成并表征了含有两个1-[2-(二乙氨基)乙基]咪唑亚基配体的新型金(I)配合物。给出了两种关键化合物的X射线结构。所有配合物均已在前列腺癌细胞系PC-3中测试其抗增殖活性。已测定了这些配合物的亲脂性(Log P)。对活性最高的配合物在五种人类癌细胞系和原代内皮细胞中进行了细胞毒性活性测试。活性最高的配合物对癌细胞表现出强效选择性。
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