Autor: |
Henryk Mastalarz, Agnieszka Mastalarz, Joanna Wietrzyk, Magdalena Milczarek, Andrzej Kochel, Andrzej Regiec |
Jazyk: |
angličtina |
Rok vydání: |
2023 |
Předmět: |
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Zdroj: |
Molecules, Vol 28, Iss 3, p 1284 (2023) |
Druh dokumentu: |
article |
ISSN: |
1420-3049 |
DOI: |
10.3390/molecules28031284 |
Popis: |
Two novel platinum(II) complexes (1 and 2) were synthesized by the reaction of the appropriate 3,5-dimethyl-4-nitroisoxazole with K2PtCl4 and characterized by elemental analysis, ESI MS spectrometry, 1H NMR and far-IR spectroscopy. The structure of trans complex 2 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 trans complex 2 showed much better cytotoxic activity than cisplatin for all the tested cancer cell lines. Cis complex 1 was inferior to its trans 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 1 and 2. |
Databáze: |
Directory of Open Access Journals |
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