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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and in vitro antitumor activity of novel iridium(III) complexes with enantiopure C2-symmetrical vicinal diamine ligands
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Synthesis and in vitro antitumor activity of novel iridium(III) complexes with enantiopure C2-symmetrical vicinal diamine ligands

机译：具有对映纯C2-对称邻二胺配体的新型铱（III）配合物的合成及体外抗肿瘤活性

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摘要

Four novel iridium(III) complexes with enantiopure C2- symmetrical vicinal diamine ligands were designed, synthesized, and characterized by FT-IR, NMR, and MS. The cytotoxicities of all of the complexes against the human solid tumor cell lines A2780, A549, KB, and MDA-MB-231 were evaluated. Both R,R-configured complexes (R,R)-5a and (R,R)-5b exhibited more potent or similar activity compared with oxaliplatin, whereas their corresponding (S,S)-isomers (S,S)-5a and (S,S)-5b were found to be mostly inactive. As indicated by the activation of caspase-3, the cleavage of PARP, and the upregulation of p53, the preliminary mechanism studies revealed that the mode of cell death initiated by (R,R)-5a in A2780 cells was predominantly p53-mediated apoptosis. In addition, the structure of (R,R)-5a was unambiguously confirmed through single crystal X-ray structure determination.
机译：通过FT-IR，NMR和MS设计，合成和表征了具有对映纯C2-对称邻二胺配体的四种新型铱（III）配合物。评估了所有复合物对人实体瘤细胞系A2780，A549，KB和MDA-MB-231的细胞毒性。与奥沙利铂相比，R，R构型的复合物（R，R）-5a和（R，R）-5b均显示出更有效的活性或相似活性，而其相应的（S，S）-异构体（S，S）-5a和发现（S，S）-5b大部分不活跃。正如caspase-3的激活，PARP的裂解和p53的上调所表明的那样，初步的机理研究表明，由（R，R）-5a引起的A2780细胞的细胞死亡模式主要是p53介导的凋亡。另外，通过单晶X射线结构测定明确地确认了（R，R）-5a的结构。

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