设计，合成，DNA / HSA绑定和含三芳基胺-硫代氨基脲杂化物的半三明治Ru（II）-芳烃配合物的细胞毒活性。,ACS Omega

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设计，合成，DNA / HSA绑定和含三芳基胺-硫代氨基脲杂化物的半三明治Ru（II）-芳烃配合物的细胞毒活性。
ACS Omega ( IF 3.7 ) Pub Date : 2019-07-05 , DOI: 10.1021/acsomega.9b01022
Mathiyan Muralisankar ₁ , Ramachandran Dheepika ₁ , Jebiti Haribabu _{2,

3} , Chandrasekar Balachandran ₃ , Shin Aoki _{3,

3} , Nattamai S P Bhuvanesh ₄ , Samuthira Nagarajan ₁

Affiliation

由于其优异的抗癌活性，有机钌络合物是铂基络合物的有效替代品。在这项研究中，报道了一系列新的具有三芳基胺-硫代半碳杂hybrid杂配体的Ru（II）-芳烃配合物，其抗癌活性高于顺铂。配体和配合物的分子结构在光谱学上得到确认，并由单晶X射线晶体学支持。这些建筑群采用了三脚钢琴凳的几何形状。使用3-（4,5-二甲基噻唑-2-基）-2,5-二苯基溴化四氮唑测定。有趣的是，带有吡咯烷的Ru（II）-苯配合物对低IC50值的癌细胞表现出优异的活性，菌落形成研究显示在5和10μM的浓度下完全抑制。此外，通过a啶橙和碘化丙啶染色评估的形态变化表明，细胞死亡是由凋亡引起的。此外，通过吸收和发射光谱法研究了合成的Ru（II）-芳烃配合物与DNA /蛋白质之间的相互作用。这些合成的新有机钌复合物可用于开发新的基于金属的抗癌药物。通过a啶橙和碘化丙啶染色评估形态学变化，表明细胞死亡是由凋亡引起的。此外，通过吸收和发射光谱法研究了合成的Ru（II）-芳烃配合物与DNA /蛋白质之间的相互作用。这些合成的新有机钌复合物可用于开发新的基于金属的抗癌药物。通过a啶橙和碘化丙啶染色评估形态学变化，表明细胞死亡是由凋亡引起的。此外，通过吸收和发射光谱法研究了合成的Ru（II）-芳烃配合物与DNA /蛋白质之间的相互作用。这些合成的新有机钌复合物可用于开发新的基于金属的抗癌药物。

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Design, Synthesis, DNA/HSA Binding, and Cytotoxic Activity of Half-Sandwich Ru(II)-Arene Complexes Containing Triarylamine-Thiosemicarbazone Hybrids.

Organoruthenium complexes are potent alternatives for platinum-based complexes because of their superior anticancer activity. In this investigation, a series of new Ru(II)-arene complexes with triarylamine-thiosemicarbazone hybrid ligands with higher anticancer activity than cisplatin are reported. The molecular structure of the ligands and complexes was confirmed spectroscopically and supported by single-crystal X-ray crystallography. These complexes adopted a three-leg piano stool geometry. All the Ru(II)-arene complexes were systematically investigated for their in vitro cytotoxicity against human cervical (HeLa S3), lung (A549) cancer, and human normal lung (IMR-90) cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Interestingly, a pyrrolidine-attached Ru(II)-benzene complex exhibited superior activity against cancer cells with low IC50 values, and colony formation study showed complete inhibition at 5 and 10 μM concentration. Furthermore, morphological changes assessed by acridine orange and propidium iodide staining revealed that the cell death occurred by apoptosis. In addition, the interaction between synthesized Ru(II)-arene complexes and DNA/protein was explored by absorption and emission spectroscopy methods. These synthesized new organoruthenium complexes can be used for developing new metal-based anticancer drugs.

更新日期：2019-07-05

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