Synthesis and Cytotoxic Activity of Cisplatin Analogue with an Ursodeoxycholate Ligand

Author(s): Martin Perez-Andres, Juan Jose Benito, Emilio Rodriguez-Fernandez, Juan Luis Manzano, Susana Barrena, Alberto Orfao, Julio Jose Criado.

Journal Name: Letters in Drug Design & Discovery

Volume 4 , Issue 5 , 2007

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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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Article Details

Year: 2007
Page: [341 - 345]
Pages: 5
DOI: 10.2174/157018007780867898
Price: $58