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首页> 外文期刊>Polyhedron: The International Journal for Inorganic and Organometallic Chemistry >Organotin complexes of pyruvic acid thiosemicarbazone: Synthesis, crystal structures and antiproliferative activity of neutral and cationic diorganotin complexes
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Organotin complexes of pyruvic acid thiosemicarbazone: Synthesis, crystal structures and antiproliferative activity of neutral and cationic diorganotin complexes

机译：丙酮酸硫半脲酮的有机锡复合物：中性和阳离子二有机锡复合物的合成，晶体结构和抗增殖活性

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摘要

The synthesis and spectral characterization of novel neutral and cationic organotin complexes with pyruvic acid thiosemicarbazone, H2Pt (1), [SnPh2(pt)] (2), [SnMe2(Hpt)(H2O)]Cl (3) and [SnPh2(Hpt)(H2O)]Cl (4) are reported. The crystal structure of the complexes [SnPh2(pt)] (2) and [SnMe2(Hpt)(H2O)]Cl (3) have been solved by single-crystal X-ray diffraction. The crystal structure of complex 2 showed that the ligand is doubly deprotonated at the oxygen and amide nitrogen atoms and is coordinated to the SnPh2 fragment via two five-membered chelate rings. The monomers of 2 are linked through intermolecular hydrogen bonds of C-H-O type and through pi-pi intermolecular interactions. The crystal structure of [SnMe2(Hpt)(H2O)]Cl (3) showed that the ligand is mono-deprotonated at the oxygen atom and is coordinated to the SnMe2 fragment via two five-membered chelate rings. The counter ion chloride is participated in intermolecular hydrogen bonds. An extended network of intermolecular hydrogen bonds leads to aggregation and a supramolecular assembly. The IR and NMR spectroscopic data of the complexes are reported. The in vitro cytotoxic activity has been evaluated against the cells of three human cancer cell lines: MCF-7: (human breast cancer cell line), T-24 (bladder cancer cell line), A-549(non-small cell lung carcinoma) and a mouse L-929 (a fibroblast-like cell line cloned from strain). The most active of all was found the diorganotin complex 2. The cytotoxic activity shown by these compounds against all these cancer cell lines indicates that coupling of 1 with R2Sn(IV) metal center result in metallic complexes with important biological properties and remarkable cytotoxic activity, since they are display IC50 values in a mu M range the same or better to that of the antitumor drug cisplatin. Compound 2 is considered as agent with potential antitumor activity, and can therefore be candidate for further stages of screening in vitro and/or in vivo.
机译：新型中性和阳离子有机锡配合物与丙酮酸硫代半脲，H2Pt（1），[SnPh2（pt）]（2），[SnMe2（Hpt）（H2O）] Cl（3）和[SnPh2（Hpt）的合成和光谱表征）（H 2 O）] Cl（4）的报道。配合物[SnPh2（pt）]（2）和[SnMe2（Hpt）（H2O）] Cl（3）的晶体结构已通过单晶X射线衍射解析。配合物2的晶体结构表明，该配体在氧和酰胺氮原子处双去质子化，并通过两个五元螯合环与SnPh2片段配位。 2的单体通过C-H-O型分子间氢键和pi-pi分子间相互作用连接。 [SnMe2（Hpt）（H2O）] Cl（3）的晶体结构表明，该配体在氧原子处被单去质子化，并通过两个五元螯合环与SnMe2片段配位。抗衡离子氯化物参与分子间氢键。分子间氢键的扩展网络导致聚集和超分子组装。报道了配合物的IR和NMR光谱数据。已经评估了对三种人类癌细胞系的细胞的体外细胞毒性活性：MCF-7 ：（人类乳腺癌细胞系），T-24（膀胱癌细胞系），A-549（非小细胞肺癌） ）和小鼠L-929（从菌株克隆的成纤维细胞样细胞系）。所有化合物中最活跃的是二有机锡复合物2。这些化合物对所有这些癌细胞系的细胞毒活性表明1与R2Sn（IV）金属中心的偶联导致金属复合物具有重要的生物学特性和显着的细胞毒活性，因为它们显示的IC50值在μM范围内，与抗肿瘤药顺铂的IC50值相同或更好。化合物2被认为是具有潜在抗肿瘤活性的试剂，因此可以作为体外和/或体内筛选的进一步阶段的候选物。

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