Institute of Inorganic Chemistry, Faculty of Chemistry, University of Vienna, Waehringer Straße 42, 1090 Vienna, Austria.
Vienna Doctoral School in Chemistry (DoSChem), Faculty of Chemistry, University of Vienna, Waehringer Straße 42, 1090 Vienna, Austria.
Dalton Trans. 2024 Mar 19;53(12):5567-5579. doi: 10.1039/d4dt00245h.
In this contribution we report the synthesis, characterization and anticancer activity of novel cyclometalated 4-phenylthiazole-derived ruthenium(II) (2a-e) and osmium(II) (3a-e) complexes. Formation and sufficient purity of the complexes were unambigiously confirmed by H-, C- and 2D-NMR techniques, X-ray diffractometry, HRMS and elemental analysis. The binding preferences of these cyclometalates to selected amino acids and to DNA models including G-quadruplex structures were analyzed. Additionally, their stability and behaviour in aqueous solutions was determined by UV-Vis spectroscopy. Their cellular accumulation, their ability of inducing apoptosis, as well as their interference in the cell cycle were studied in SW480 colon cancer cells. The anticancer potencies were investigated in three human cancer cell lines and revealed IC values in the low micromolar range, in contrast to the biologically inactive ligands.
在本研究中，我们报告了新型偕二茂铁 4-苯基噻唑衍生的钌(II)（2a-e）和锇(II)（3a-e）配合物的合成、表征和抗癌活性。通过 H-、C-和 2D-NMR 技术、X 射线衍射、高分辨率质谱和元素分析明确证实了配合物的形成和足够的纯度。分析了这些金属环戊二烯基与选定的氨基酸以及包括 G-四链体结构在内的 DNA 模型的结合偏好。此外，通过紫外可见光谱法测定了它们在水溶液中的稳定性和行为。在 SW480 结肠癌细胞中研究了它们的细胞积累、诱导细胞凋亡的能力以及对细胞周期的干扰。在三种人类癌细胞系中研究了它们的抗癌效力，结果表明其 IC 值在低微摩尔范围内，与生物活性较低的配体相比。
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