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[(p-cym)RuX(pz4lut)]n+ 和 [{(p-cym)RuX}2(μ-pz4lut)]n+(X = Cl、H2O 和 pz4lut = α,α,α',α'-四(吡唑-1-基)-2,6- 卢定)的合成、表征及生物活性。

Synthesis, characterisation and biological activities of [(p-cym)RuX(pz4lut)]n+ and [{(p-cym)RuX}2(μ-pz4lut)]n+ (X = Cl, H2O and pz4lut = α,α,α',α'-tetra(pyrazol-1-yl)-2,6-lutidine).

机构信息

School of Basic Sciences, Indian Institute of Technology Bhubaneswar, Bhubaneswar, Orissa-751007, India.

出版信息

Dalton Trans. 2013 Oct 21;42(39):14081-91. doi: 10.1039/c3dt51275d.

DOI:10.1039/c3dt51275d
PMID:23938874
Abstract

Mononuclear [(p-cym)RuCl(pz4lut)]Cl (1) and dinuclear [{(p-cym)RuCl}2(μ-pz4lut)]Cl2 (2) complexes (p-cym = 1-isopropyl-4-methylbenzene) comprising of bis(pyrazol-1-yl)methane based heteroscorpionate ligand α,α,α′,α′-tetra(pyrazol-1-yl)-2,6-lutidine (pz4lut) have been synthesised from pz4lut ligand and dimeric precursor complex [(p-cym)RuCl(μ-Cl)]2 in methanol. The aqua derivatives (p-cym)Ru(H2O)(pz4lut)2 (3) and {(p-cym)Ru(H2O)}2(μ-pz4lut)4 (4) are obtained from 1 and 2, respectively, via Cl/H2O exchange process in presence of appropriate equivalents of AgClO4 in methanol–water mixture. The molecular structures of dinuclear complexes, 2 and 4 are authenticated by their single crystal X-ray structures. Cyclic voltammetry reveals negligible electronic communication between the metal centres in the ligand bridged complex 2. All four complexes have been tested for their anticancer activities in human breast (MCF7), lung (A549) and colon (HCT116) cancer cell lines. The complexes show dose dependent suppression of cell viability with moderately good IC50 values ranging from 3.5–92 μM. Experimental results have revealed that the aqua derivatives, 3 and 4 exhibit better cytotoxic effect against all those cell lines as compared to the precursor chlorido complexes, 1 and 2. Results also demonstrate that the complexes are more potent against HCT116 cells as compared to other cell lines.

摘要

单核 [(p-cym)RuCl(pz4lut)]Cl(1)和双核 [{(p-cym)RuCl}2(μ-pz4lut)]Cl2(2)配合物(p-cym = 1-异丙基-4-甲基苯)由基于双(吡唑-1-基)甲烷的异噁唑啉配体α,α,α′,α′-四(吡唑-1-基)-2,6- 卢定(pz4lut)和二聚体前体配合物 [(p-cym)RuCl(μ-Cl)]2 在甲醇中合成。水合衍生物 (p-cym)Ru(H2O)(pz4lut)2(3)和 {(p-cym)Ru(H2O)}2(μ-pz4lut)4(4)分别由 1 和 2 通过 Cl/H2O 交换过程在甲醇-水混合物中使用适当当量的 AgClO4 获得。双核配合物 2 和 4 的分子结构通过单晶 X 射线结构得到证实。循环伏安法表明配体桥联配合物 2 中金属中心之间几乎没有电子通信。所有四个配合物都在人乳腺癌(MCF7)、肺癌(A549)和结肠癌(HCT116)癌细胞系中进行了抗癌活性测试。这些配合物表现出剂量依赖性的细胞活力抑制,其 IC50 值在 3.5-92 μM 之间。实验结果表明,与前体氯代配合物 1 和 2 相比,水合衍生物 3 和 4 对所有这些细胞系表现出更好的细胞毒性作用。结果还表明,与其他细胞系相比,这些配合物对 HCT116 细胞更有效。

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