Diruthenium(II,III) metal-metal multiply bonded paddlewheel complexes bearing non-steroidal anti-inflammatory drugs are promising anticancer metallodrugs. The [Ru₂(Ibp)₄Cl] (Ibp, ibuprofenate anion from HIbp ibuprofen drug), free or encapsulated, shows anticancer activity against glioblastoma (in vitro, in vivo), and against human breast and prostate cancer cells. Herein we report the interaction of [Ru₂(Ibp)₄Cl] and of [Ru₂(Ac)₄(H₂O)₂]PF₆ (Ac, acetate) with the 4-aminopyridine (4Apy) drug. The N-ligand was capable of cleaving the paddlewheel unit with oxidation of Ru₂(II,III) to Ru₂(III,III)O μ-oxo core in the ibuprofen complex while the acetate complex underwent axial substitution of water by 4Apy. Carefully designed synthetic and chromatographic methods succeeded in giving the novel [Ru₂O(Ibp)₂(4Apy)₆]Cl₂ metallodrug, the first diruthenium(III,III) μ-oxo having chloride as counterion. Characterization was performed by elemental analysis, mass spectrometry, thermogravimetric analysis, electronic absorption and vibrational spectroscopies, molar conductivity and cyclic voltammetry. Kinetic studies for the μ-oxo complex (in 50:50 v/v ethanol:water) suggested an aquation/complexation equilibrium in consecutive step reactions with the exchange of the two 4Apy trans to the μ-oxo bridge by water (aquation) and the back coordination of 4Apy in excess of the N-ligand (complexation). Trypan blue assays for the novel compound showed time- and dose- dependent antiproliferative effects (at 5–50 μmol L⁻¹) and cytotoxicity (> 20 μmol L⁻¹), and MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) assays gave IC₅₀ value of 7.6 ± 1.5 μmol L⁻¹ (at 48 h, 1–20 μmol L⁻¹) against U87MG human glioblastoma cells (aggressive brain glioma cancer) pointing the metallodrug as potential candidate for novel therapies in gliomas.

含有非甾体抗炎药的二钌(II,III)金属-金属多重键合桨轮配合物是很有前景的抗癌金属药物。[Ru ₂ (Ibp) ₄ Cl]（Ibp，来自 HIbp 布洛芬药物的布洛芬酸阴离子），游离的或包封的，对胶质母细胞瘤（体外、体内）以及人乳腺癌和前列腺癌细胞具有抗癌活性。在此我们报告了[Ru ₂ (Ibp) ₄ Cl] 和[Ru ₂ (Ac) ₄ (H ₂ O) ₂ ]PF ₆ (Ac, 醋酸盐) 与4-氨基吡啶(4Apy) 药物的相互作用。N __{-配体能够通过将布洛芬络合物中的Ru 2} (II,III)氧化为Ru ₂ (III,III)O μ-oxo核心来切割桨轮单元，而乙酸络合物通过4Apy轴向取代水。精心设计的合成和色谱方法成功地得到了新的[Ru ₂ O(Ibp) ₂ (4Apy) ₆ ]Cl ₂金属药物，第一个二钌（III，III）μ-氧代具有氯化物作为抗衡离子。通过元素分析、质谱、热重分析、电子吸收和振动光谱、摩尔电导率和循环伏安法进行表征。μ-oxo 复合物（在 50:50 v/v 乙醇：水中）的动力学研究表明，在连续步骤反应中水化/络合平衡，两个 4Apy反式通过水交换到 μ-氧桥（水化）和4Apy 的后配位超过N-配体（络合）。新型化合物的台盼蓝试验显示出时间和剂量依赖性抗增殖作用（在 5-50 μmol L ^-1时）和细胞毒性（> 20 μmol L ^-1) 和 MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) 测定的 IC ₅₀值为 7.6 ± 1.5 μmol L ^-1（在 48 小时，1– 20 μmol L ^-1 ) 对抗 U87MG 人胶质母细胞瘤细胞（侵袭性脑胶质瘤）表明该金属药物是胶质瘤新疗法的潜在候选者。