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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Synthesis, antiradical activity and in vitro cytotoxicity of novel organotin complexes based on 2,6-di-tert-butyl-4-mercaptophenol
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Synthesis, antiradical activity and in vitro cytotoxicity of novel organotin complexes based on 2,6-di-tert-butyl-4-mercaptophenol

机译：基于2,6-二叔丁基-4-巯基苯酚的新型有机锡配合物的合成，抗自由基活性和体外细胞毒性

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摘要

A series of organotin complexes with Sn-S bonds of formulae Me_2Sn(SR)_2 (1); Et_2Sn(SR)_2 (2); (n-Bu)_2Sn-(SR)_2 (3); Ph_2Sn(SR)_2 (4); R_2Sn(SR)_2 (5); Me_3SnSR (6); Ph_3SnSR (7) (R = 3,5-di-tert-butyl-4-hydroxyphenyl) were synthesized and characterized by elemental analysis, ~1H, ~(13)C NMR, and IR. The crystal structures of compounds 1, 4, 5, and 7 were determined by X-ray diffraction analysis. The tetrahedral geometry around the Sn center in the monocrystals of 1, 4, 5, and 7 was confirmed by X-ray crystallography. The high radical scavenging activity of the complexes was confirmed spectrophotometrically in a DPPH-test. The binding affinity of 1-7 and the starting R_2SnCl_2 (8) towards tubulin through their interaction with SH groups of proteins was studied. It was found that the hindered organotin complexes could interact with the colchicine site of tubulin, which makes them promising antimitotic drugs. Compounds 1-8 were tested for their in vitro cytotoxicity against human breast (MCF-7) and human cervix (HeLa) adenocarcinoma cells. Complexes 1-8 were also tested against normal human fetal lung fibroblast cells(MRC-5). Complexes 2-4 and 8 exhibit significantly lower cytostatic activity against the normal MRC-5 cell line compared to the tumor cell lines MCF-7 and HeLa used. A high activity against both cell lines 250 nM (MCF-7) and 160 nM (HeLa) was determined for the triphenyltin complex 7 while the introduction of hindered phenol groups decreases the cytotoxicity of the complexes against normal cells.
机译：一系列具有式Me_2Sn（SR）_2的Sn-S键的有机锡配合物（1）; Et_2Sn（SR）_2（2）; （n-Bu）_2Sn-（SR）_2（3）; Ph_2Sn（SR）_2（4）; R_2Sn（SR）_2（5）; Me_3SnSR（6）;合成了Ph_3SnSR（7）（R = 3,5-二叔丁基-4-羟基苯基），并通过元素分析，〜1H，〜（13）C NMR和IR对其进行了表征。通过X射线衍射分析确定化合物1、4、5和7的晶体结构。通过X射线晶体学确认在1、4、5和7的单晶中Sn中心周围的四面体几何形状。在DPPH测试中通过分光光度法确认了复合物的高自由基清除活性。研究了1-7和起始R_2SnCl_2（8）通过与SH蛋白基团的相互作用对微管蛋白的结合亲和力。发现受阻的有机锡复合物可以与微管蛋白的秋水仙碱位点相互作用，这使它们成为有前途的抗有丝分裂药物。测试了化合物1-8对人乳腺（MCF-7）和人宫颈（HeLa）腺癌细胞的体外细胞毒性。还测试了复合物1-8对正常人胎儿肺成纤维细胞（MRC-5）的作用。与所使用的肿瘤细胞系MCF-7和HeLa相比，复合物2-4和8对正常MRC-5细胞系表现出明显更低的细胞抑制活性。对于三苯基锡复合物7，确定了针对两种细胞系250 nM（MCF-7）和160 nM（HeLa）的高活性，而引入受阻酚基团则降低了该复合物对正常细胞的细胞毒性。

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