Copper(I) and copper(II) complexes of 5-nitroimidazole conjugated heteroscorpionate ligands have been synthesized. In particular, the new 2,2-bis(pyrazol-1-yl)-N-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl)acetamide ligand (L^HMN) was synthesized by direct coupling of preformed side chain acid with 5-nitroimidazole and its coordination chemistry was investigated towards Cu(I) and Cu(II) acceptors and compared with that of the related 2,2-bis(3,5-dimethyl-1-H-pyrazol-1-yl)-N-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl)acetamide ligand (L^MeMN). The copper(II) complexes {[(L^MeMN)₂Cu]Cl₂} and {[(L^HMN)₂Cu]Cl₂} were prepared by the reaction of CuCl₂·2H₂O with L^HMN or L^MeMN ligands in methanol solution. The water soluble copper(I) complexes {[(L^MeMN)Cu(PTA)₂]}(PF₆) and {[(L^HMN)Cu(PTA)₂]}(PF₆) were prepared by the reaction of Cu(CH₃CN)₄PF₆ and 1,3,5-triaza-7-phosphaadamantane (PTA) with L^HMN or L^MeMN ligands in acetonitrile solution. The new Cu(I) and Cu(II) complexes as well as the corresponding uncoordinated ligands were evaluated for their cytotoxic activity against 2D monolayer cultures of multiple human cancer cell lines and 3D-cultured HCT-15 colon cancer spheroids. Morphological analysis by Transmission Electron Microscopy (TEM) revealed the induction of a massive cytoplasmic vacuolization consistent with a paraptotic-like cancer cell death.

已经合成了5-硝基咪唑共轭的异蝎子配体的铜（I）和铜（II）配合物。特别地，新的2,2-双（吡唑-1-基）-N-（2-（2-甲基-5-硝基-1H-咪唑-1-基）乙基）乙酰胺的配体（L ^ħ MN）为研究了通过预形成的侧链酸与5-硝基咪唑的直接偶联合成的铜及其配位化学对Cu（I）和Cu（II）受体的影响，并与相关的2,2-双（3,5-二甲基-1）进行了比较-H-吡唑-1-基）-N-（2-（2-甲基-5-硝基-1H-咪唑-1-基）乙基）乙酰胺配体（L ^Me MN）。铜（II）络合物{[（L ^Me MN）₂ Cu] Cl ₂ }和{[（L ^H MN）₂ Cu] Cl ₂通过在甲醇溶液中使CuCl ₂ ·2H ₂ O与L ^H MN或L ^Me MN配体反应制备。通过反应制备水溶性铜（I）络合物{[（L ^Me MN）Cu（PTA）₂ ]}（PF ₆）和{[（L ^H MN）Cu（PTA）₂ ]}（PF ₆）。L ^H MN或L ^Me制备Cu（CH ₃ CN）₄ PF ₆和1,3,5-三氮杂-7-磷金刚烷（PTA）乙腈溶液中的MN配体。评估了新的Cu（I）和Cu（II）配合物以及相应的未配位配体对多种人类癌细胞系和3D培养的HCT-15结肠癌球体的2D单层培养物的细胞毒活性。透射电子显微镜（TEM）的形态学分析显示，诱导了大量细胞质空泡化，与拟态性的癌细胞死亡一致。