Four platinum(II) complexes of general formula [PtCl(g1-C9H7)L2] [where L2 is 1,2-bis(diphenylphosphino) ethane (dppe) 1 or cycloocta-1,5-diene (cod) 3] and [PtCl2L2] (where L2 is dppe 2 or cod 4) were studied. Inhibition growth assays on human tumor cell lines evidenced for 1 and 3 an antiproliferative effect and, interestingly, the cytotoxic effect exerted by 1 is similar to that of cisplatin. Electrochemical and NMR measurements allowed us to determine the structural and redox properties. Investigation of the mechanism of action responsible for the cytotoxicity demonstrated a weak capacity of interacting with DNA. Some experiments performed on rat liver mitochondria indicate that 1 acts as an inducer of the mitochondrial permeability transition, thus leading to the release of proapoptotic factors, such as cytochrome c and apoptosis-inducing factor.

Platinum(II)-Chloride Indenyl Complexes: Electrochemical and Biological Evaluation

DALLA VIA, LISA;SANTI, SAVERIO;DI NOTO, VITO;TONINELLO, ANTONIO
2011

Abstract

Four platinum(II) complexes of general formula [PtCl(g1-C9H7)L2] [where L2 is 1,2-bis(diphenylphosphino) ethane (dppe) 1 or cycloocta-1,5-diene (cod) 3] and [PtCl2L2] (where L2 is dppe 2 or cod 4) were studied. Inhibition growth assays on human tumor cell lines evidenced for 1 and 3 an antiproliferative effect and, interestingly, the cytotoxic effect exerted by 1 is similar to that of cisplatin. Electrochemical and NMR measurements allowed us to determine the structural and redox properties. Investigation of the mechanism of action responsible for the cytotoxicity demonstrated a weak capacity of interacting with DNA. Some experiments performed on rat liver mitochondria indicate that 1 acts as an inducer of the mitochondrial permeability transition, thus leading to the release of proapoptotic factors, such as cytochrome c and apoptosis-inducing factor.
2011
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11577/2480561
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