未修饰的桨轮二价二乙酸根/甲酰胺基合铑(II,II)配合物及其轴向修饰的低价金属树状大分子的细胞毒性评价。
Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers.
机构信息
Department of Chemistry, University of Cape Town, Rondebosch, Cape Town 7701, South Africa.
Tumour Biology Department, The Oncology Institute "Prof. Dr. Ion Chiricuţă", 400015 Cluj-Napoca, Romania.
出版信息
Molecules. 2023 Mar 15;28(6):2671. doi: 10.3390/molecules28062671.
Two diphenyl formamidine ligands, four dirhodium(II,II) complexes, and three axially modified low-valent dirhodium(II,II) metallodendrimers were synthesized and evaluated as anticancer agents against the A2780, A2780, and OVCAR-3 human ovarian cancer cell lines. The dirhodium(II,II) complexes show moderate cytotoxic activity in the tested tumor cell lines, with acetate and methyl-substituted formamidinate compounds displaying increased cytotoxicity that is relative to cisplatin in the A2780 cisplatin resistant cell line. Additionally, methyl- and fluoro-substituted formamidinate complexes showed comparable and increased cytotoxic activity in the OVCAR-3 cell line when compared to cisplatin. The low-valent metallodendrimers show some activity, but a general decrease in cytotoxicity was observed when compared to the precursor complexes in all but one case, which is where the more active acetate-derived metallodendrimer showed a lower IC value in the OVCAR-3 cell line in comparison with the dirhodium(II,II) tetraacetate.
合成了两种二苯甲脒配体、四种二价铑（II，II）配合物和三种轴向修饰的低价二价铑（II，II）金属树状大分子，并将其作为抗癌剂评估对 A2780、A2780 和 OVCAR-3 人卵巢癌细胞系的作用。二价铑（II，II）配合物在测试的肿瘤细胞系中表现出中等细胞毒性活性，其中乙酸盐和甲基取代的甲脒化合物显示出与顺铂在 A2780 顺铂耐药细胞系中的相对增加的细胞毒性。此外，与顺铂相比，甲基和氟取代的甲脒配合物在 OVCAR-3 细胞系中显示出相当和增加的细胞毒性活性。低价金属树状大分子显示出一些活性，但与前体配合物相比，除了一种情况外，一般观察到细胞毒性降低，其中更具活性的乙酸盐衍生的金属树状大分子在 OVCAR-3 细胞系中的 IC 值低于二价铑（II，II）四乙酸盐。
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