Synthesis and Cytotoxic Activity of Cisplatin Analogue with an Ursodeoxycholate Ligand
Juan Jose Benito,
Juan Luis Manzano,
Julio Jose Criado.
New cisplatin analogue carrying a cholic acid, complex [PtCl(UDC)(en)] (en = ethylenediamine, UDC = Ursodeoxycholate) has been synthesized from [PtCl2(en)] and characterized. This novel complex shows increased cytotoxicity against a cisplatin-resistant ovarian tumor cell line (CH1cisR) as compared with the parent compound cisDDP. Moreover, while cisplatin only exerts its activity over the G2/M population, [PtCl(UDC)(en)] seems to induce apoptosis both in cycling and resting cells. Intrinsically fluorescence at room temperature was observed for this platinum complex with a quantum yield φ = 0.11. In order to achieve dynamic pictures of the biological effects of cisplatin analogues, it would be very interesting to have intrinsically fluorescent compounds with cytotoxic activity, especially against drug-resistant cell-lines.
Keywords: Autofluorescent Pt(II) complexes, Shuttle compounds, Cytotoxic activity, Bile acids
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