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  • Platinum(II) Complexes Bearing Triphenylphosphine and Chelating Oximes: Antiproliferative Effect and Biological Profile in Resistant Cells.

Platinum(II) Complexes Bearing Triphenylphosphine and Chelating Oximes: Antiproliferative Effect and Biological Profile in Resistant Cells.

ChemMedChem (2020-06-04)
Mariafrancesca Hyeraci, Marialuigia Colalillo, Luca Labella, Fabio Marchetti, Simona Samaritani, Valeria Scalcon, Maria Pia Rigobello, Lisa Dalla Via
ABSTRACT

Platinum(II) complexes of the type [Pt(Cl)(PPh3 ){(κ2 -N,O)-(1{C(R)=N(OH)-2(O)C6 H4 })}] with R=Me, H, (1 and 2) were synthesized and characterized. Single-crystal X-ray diffraction confirmed the proposed (SP4-3) configuration for 1. Study of the antiproliferative activity, performed on a panel of human tumor cell lines and on mesothelial cells, highlighted complex 2 as the more effective. In particular, it showed a remarkable cytotoxicity in ovarian carcinoma cells (A2780) and interestingly, a significant antiproliferative effect on cisplatin resistant cells (A2780cis). Investigation into the intracellular mechanism of action demonstrated that 2 had a lower ability to platinate DNA than did cisplatin, which was taken as reference, and a notably higher uptake in resistant cells. A significant accumulation in mitochondria, along with the ability to induce concentration-dependent mitochondrial membrane depolarization and intracellular reactive oxygen species production, allowed us to propose a mitochondrion-mediated pathway as responsible for the interesting cytotoxic profile of complex 2.

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RPMI-1640 Medium, With L-glutamine, without sodium bicarbonate, powder, suitable for cell culture
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Deoxyribonucleic acid sodium salt from salmon testes
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Nutrient Mixture F-12 Ham, Kaighn′s Modification, with L-glutamine, without sodium bicarbonate, powder, suitable for cell culture
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
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100 μL
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
$515.00
0.2 mL
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
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Sigma-Aldrich
Nutrient Mixture F-12 Ham, With L-glutamine, without sodium bicarbonate, powder, suitable for cell culture
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SKUPack SizeAvailabilityPriceQuantity
25 μL
In Stock
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
$179.00
100 μL
In Stock
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
$515.00
0.2 mL
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Details...
A recombinant, preservative-free antibody is available for your target. Try ZRB1151
$678.00
$555.96
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Antibiotic Antimycotic Solution (100×), Stabilized, with 10,000 units penicillin, 10 mg streptomycin and 25 μg amphotericin B per mL, 0.1 μm filtered, BioReagent, suitable for cell culture
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25 μL
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
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100 μL
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A recombinant, preservative-free antibody is available for your target. Try ZRB1151
$515.00
0.2 mL
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Details...
A recombinant, preservative-free antibody is available for your target. Try ZRB1151
$678.00
$555.96