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Synthesis of platinum(II) complexes with some 1-methylnitropyrazoles and in vitro research on their cytotoxic activity.
Autorzy
Rok wydania
2020
Czasopismo
Numer woluminu
13
Strony
433/1-433/21
DOI
10.3390/ph13120433
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
Streszczenie
A series of eight novel platinum(II) complexes were synthesized by the reaction of the appropriate 1-methylnitropyrazole derivatives with K2PtCl4 and characterized by elemental analysis, ESI MS spectrometry, 1H NMR, 195Pt NMR, IR and far IR spectroscopy. Thermal isomerization of cis-dichloridobis(1-methyl-4-nitropyrazole)platinum(II) 1 to trans-dichloridobis(1-methyl-4-nitropyrazole)platinum(II) 2 has been presented, and the structure of the compound 2 has been confirmed by X-ray diffraction method. 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) and their logP was measured using a shake-flask method. The trans complex 2 showed better antiproliferative activity than cisplatin for all the tested cancer cell lines. Additionally, trans-dichloridobis(1-methyl-5-nitropyrazole)platinum(II) 4 has featured a lower IC50 value than reference cisplatin against MCF-7 cell line. To gain additional information that may facilitate the explanation of the mode of action of tested compounds cellular platinum uptake, stability in L-glutathione solution, influence on cell cycle progression of HL-60 cells and ability to apoptosis induction were determined for compounds 1 and 2.
Słowa kluczowe
nitropyrazoles-Pt(II)complexes, synthesis, structural analysis, LogP, cellular platinum uptake, antiproliferative activity, normoxia-hypoxia, L-glutathione (GSH), cell cycle, X-ray crystallography
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Pełny tekst licencji: https://creativecommons.org/licenses/by/3.0/pl/legalcode
Adres publiczny
http://dx.doi.org/10.3390/ph13120433
Strona internetowa wydawcy
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