Tin thiocarbonohydrazone complexes: synthesis, crystal structures and biological evaluation.,Toxicology Research

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Tin thiocarbonohydrazone complexes: synthesis, crystal structures and biological evaluation.
Toxicology Research ( IF 2.2 ) Pub Date : 2019-08-30 , DOI: 10.1039/c9tx00109c
Jin Wang ₁ , Yu-Ting Wang ₂ , Yan Fang ₃ , Yan-Li Lu ₃ , Ming-Xue Li ₃

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In this article, three organotin complexes formulated as [(Me)2Sn(H2L1)] (1), [(Ph)2Sn(H2L1)]·MeOH (2) and [(Me)2Sn(HL2)(OAc)]4(Me)2O (3) (H4L1 = bis(2-hydroxybenzaldehyde) thiocarbohydrazone and H2L2 = bis(2-acetylpyrazine) thiocarbonohydrazone) have been synthesized and structurally characterized. Growth inhibition assays indicated that both the proligands and the three complexes are capable of showing anticancer activity against the human hepatocellular carcinoma HepG2 cells with H2L2 and complex 3 showing much higher cytotoxic potential. Subsequent toxicity studies on normal QSG7701cells showed that complex 3 has the highest tumor cell selectivity, and its IC50 value on QSG7701 cells is 8.48 fold higher than that in HepG2 cells. In acute toxicity experiments, complex 3 produces a dose-dependent effect in NIH mice with a LD50 value of 17.2 mg kg-1.

中文翻译：

锡硫代碳腙配合物：合成、晶体结构和生物学评价。

在本文中，三种有机锡配合物分别表示为 [(Me)2Sn(H2L1)] (1)、[(Ph)2Sn(H2L1)]·MeOH (2) 和 [(Me)2Sn(HL2)(OAc)]4 (Me)2O (3) (H4L1 = 双(2-羟基苯甲醛) 硫代羰腙和H2L2 = 双(2-乙酰吡嗪) 硫代羰腙) 已被合成并在结构上进行了表征。生长抑制测定表明，前配体和三种复合物都能够对人肝细胞癌 HepG2 细胞显示出抗癌活性，而 H2L2 和复合物 3 显示出更高的细胞毒性潜力。随后对正常QSG7701细胞的毒性研究表明，复合物3对肿瘤细胞的选择性最高，其对QSG7701细胞的IC50值是HepG2细胞的8.48倍。在急性毒性实验中，复合物 3 在 NIH 小鼠中产生剂量依赖性效应，LD50 值为 17。

更新日期：2019-08-30

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