Microwave synthesis of mixed ligand diimine-thiosemicarbazone complexes of ruthenium(II): biophysical reactivity and cytotoxicity.
Microwave synthesis of mixed ligand diimine-thiosemicarbazone complexes of ruthenium(II): biophysical reactivity and cytotoxicity.
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DOI：
10.1039/b915081a
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发表时间：
2009-12-28
期刊：
影响因子：
--
通讯作者：
Seeram NP
中科院分区：
文献类型：
--
作者：
Beckford FA;Shaloski M Jr;Leblanc G;Thessing J;Lewis-Alleyne LC;Holder AA;Li L;Seeram NP
采用一种新的微波辅助合成方法合成了一系列含有二亚胺和双齿硫代氨基脲的混合配体钌（ii）化合物。该化合物含有二亚胺1,10-菲罗啉（phen）或2,2 ' -联吡啶（bpy），硫代氨基脲是由9-蒽醛衍生而来。根据元素分析和光谱数据，化合物的最佳配方为[(phen)2Ru（硫代氨基脲）](PF6)2和[(phen)2Ru（硫代氨基脲）](PF6)2，其中硫代氨基脲= 9-蒽醛-氨基硫代氨基脲，9-蒽醛- n(4)-甲基硫代氨基脲和9-蒽醛- n(4)-乙基硫代氨基脲。与溴化乙啶的荧光竞争研究以及粘度测量表明，配合物通过插入模式相对强烈地结合小牛胸腺DNA (CTDNA)，可能涉及二亚胺配体的芳香环。该复合物对MCF-7和MDA-MB-231（乳腺腺癌）以及HCT 116和HT-29（结直肠癌）细胞系显示出良好的细胞毒性。
A novel microwave-assisted synthetic method has been used to synthesise a series of mixed ligand ruthenium(ii) compounds containing diimine as well as bidentate thiosemicarbazone ligands. The compounds contain the diimine 1,10-phenanthroline (phen) or 2,2′-bipyridine (bpy) and the thiosemicarbazone is derived from 9-anthraldehyde. Based on elemental analyses and spectroscopic data, the compounds are best formulated as [(phen)2Ru(thiosemicarbazone)](PF6)2 and [(phen)2Ru(thiosemicarbazone)](PF6)2 where thiosemicarbazone = 9-anthraldehydethiosemicarbazone, 9-anthraldehyde-N(4)-methylthiosemicarbazone, and 9-anthraldehyde-N(4)-ethylthiosemicarbazone. Fluorescence competition studies with ethidium bromide, along with viscometric measurements suggests that the complexes bind calf thymus DNA (CTDNA) relatively strongly via an intercalative mode possibly involving the aromatic rings of the diimine ligands. The complexes show good cytotoxic profiles against MCF-7 and MDA-MB-231 (breast adenocarcinoma) as well as HCT 116 and HT-29 (colorectal carcinoma) cell lines.
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