Department of Organic Chemistry and Drug Technology, Faculty of Pharmacy, Wrocław Medical University, 211A Borowska Street, 50-556 Wrocław, Poland.
Faculty of Chemistry, The University of Wrocław, 14F Joliot-Curie Street, 50-383 Wrocław, Poland.
Molecules. 2023 Jan 28;28(3):1284. doi: 10.3390/molecules28031284.
Two novel platinum(II) complexes ( and ) were synthesized by the reaction of the appropriate 3,5-dimethyl-4-nitroisoxazole with KPtCl and characterized by elemental analysis, ESI MS spectrometry, H NMR and far-IR spectroscopy. The structure of complex was additionally confirmed by X-ray diffraction. The cytotoxicity of the investigated compounds was examined in vitro on three human cancer cell lines (MCF-7 breast, ES-2 ovarian and A-549 lung adenocarcinomas) in both normoxia and hypoxia conditions. LogPs of complexes were measured using the shake-flask method. The complex showed much better cytotoxic activity than cisplatin for all the tested cancer cell lines. complex was inferior to its isomer against all the cancer lines tested in normoxia conditions but proved superior to the reference cisplatin against the MCF-7 and A549 lines, and showed similar activity to cisplatin against the ES-2 line. To gain additional information that may facilitate the explanation of the pharmacological activity of the tested compounds, cellular platinum uptake and stability in L-glutathione solution were determined for both compounds and .
两个新的铂（II）配合物（和）通过适当的 3,5-二甲基-4-硝基异恶唑与 KPtCl 的反应合成，并通过元素分析、ESI MS 光谱、H NMR 和远红外光谱进行了表征。复合物的结构通过 X 射线衍射进一步证实。在常氧和缺氧条件下，在三种人癌细胞系（MCF-7 乳腺癌、ES-2 卵巢癌和 A-549 肺腺癌）中体外研究了这些化合物的细胞毒性。使用摇瓶法测量了复合物的 LogPs。与顺铂相比，复合物在所有测试的癌细胞系中均显示出更好的细胞毒性活性。在常氧条件下，复合物不如其异构体针对所有测试的癌细胞系，但对 MCF-7 和 A549 系优于参考顺铂，对 ES-2 系的活性与顺铂相似。为了获得可能有助于解释测试化合物药理活性的额外信息，确定了两种化合物和在 L-谷胱甘肽溶液中的细胞内铂摄取和稳定性。
