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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Synthesis of heterobimetallic gold(i) ferrocenyl-substituted 1,2,3-triazol-5-ylidene complexes as potential anticancer agents
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Synthesis of heterobimetallic gold(i) ferrocenyl-substituted 1,2,3-triazol-5-ylidene complexes as potential anticancer agents

机译：作为潜在的抗癌剂的杂二聚金（I）二氯联苯 - 取代的1,2,3-三唑-5-百萘络合物的合成

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摘要

1,2,3-Triazol-5-ylidene (trz) complexes of gold(i) containing a ferrocenyl substituent on the C4-position of the trz ring were synthesized to yield the neutral heterobimetallic gold(i) trz chlorido (2), gold(i) trz phenyl (3), and the cationic gold(i) trz triphenylphospine (5) complexes. In order to compare the effect of silver(i) as central metal vs. gold(i), [Ag(trz)(2)](+) (4) was also prepared, while variation of the C4-1,2,3-triazol-5-ylidene substituent from a ferrocenyl to a phenyl group was done to prepare the monometallic analogue of 5, namely the cationic Au(i) trz triphenylphosphine complex 6. The complexes were characterised with spectroscopic and electrochemical methods, and the single crystal X-ray structures of 2-6 were determined. NMR stability studies of 5 as a representative example of the series of complexes were performed to confirm the stability of the complexes in the solvent dimethylsulfoxide and in aqueous solution. The anti-cancer potential of 5 was evaluated against the lung cancer cell lines A549 and H1975, and the human embryonic kidney cell line (HEK-293) was used as a non-cancer model. IC50 values of 0.89, 0.23 and 5.43 M, respectively, were obtained for A549, H1975 and HEK-293, respectively, indicating the activity and selectivity of 5 for cancer cells. Fluorescence microscopy experiments as a preliminary mode-of-action study evidenced an apoptotic cell death mechanism rather than necrotic cell death.
机译：1,2,3-三唑-5- ylidene（Trz）含有含有铁烯基取代基的金（I）的C4-位置上的金属烯基取代基，得到中性偏异性金属金（I）Trz Hlorido（2），金（I）Trz苯基（3），以及阳离子金（I）TRZ三苯基骨折（5）配合物。为了比较银（I）作为中枢金属与金（I）的作用，还制备[Ag（Trz）（2）]（+）（4），同时C4-1,2的变异，从二氯联苯到苯基的3-三唑-5- ylidene取代基制备5，即阳离子Au（i）Trz三苯基膦络合物6.用光谱和电化学方法表征复合物，并单一确定了2-6的晶体X射线结构。进行5作为该系列复合物的代表性实例的NMR稳定性研究以确认溶剂二甲基硫氧化物和水溶液中配合物的稳定性。针对肺癌细胞系A549和H1975评价5的抗癌潜力，使用人胚胎肾细胞系（HEK-293）作为非癌症模型。分别为A549，H1975和HEK-293获得0.89,0.23和5.43m的IC 50值，表明癌细胞的活性和选择性为5。荧光显微镜实验作为初步动作模式研究证明了凋亡细胞死亡机制而不是坏死性细胞死亡。

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