Antitumor activity of a new platinum(II) complex with low nephrotoxicity and genotoxicity

Chemico-biological Interactions
C MarzanoDolores Fregona

Abstract

Cisplatin is an important antineoplastic agent, but dose-limiting nephrotoxicity and the occurrence of cellular resistance prevent its potential efficacy. Moreover, cisplatin is known to be carcinogenic and genotoxic in mammalian cells and this feature is of a special interest due to the risk of inducing secondary malignancies. There is a great interest in developing new platinum agents that have broad spectrum of antitumor activity and reduced toxicity. We have recently synthesized a novel platinum(II) coordination complex containing a pyridine nucleus and a dithiocarbamate moiety as ligands, [Pt(ESDT)(Py)Cl], in order to obtain an agent with more favorable therapeutic indices than cisplatin. In this study, the new platinum(II) complex was tested for its cytotoxicity, by MTT assay, on various human cancer cell lines also including different cisplatin-resistant cells endowed with different mechanisms of resistance. On human peripheral blood lymphocytes we evaluated the genotoxic potential of [Pt(ESDT)(Py)Cl] via micronuclei and SCE detection. We also performed in vivo experiments with the purpose of investigating the antitumor and nephrotoxic effects of the new platinum(II) complex. The antitumor activity was studied in ascitic...Continue Reading

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Citations

May 7, 2013·Chinese Medicine·Fotini PapachristouAlexandra K Tsaroucha
Jun 12, 2013·Toxicology·Xuhui TongLiang Tao
May 16, 2009·Mutation Research·Farah Maria Drumond ChequerDanielle Palma de Oliveira
Mar 9, 2010·International Journal of Cancer. Journal International Du Cancer·Lara CattaruzzaDonatella Aldinucci
Sep 21, 2010·International Journal of Cancer. Journal International Du Cancer·Cristina MarzanoDolores Fregona
Mar 21, 2007·Chemico-biological Interactions·Carla Silva Rodrigues MenezesElisângela de Paula Silveira-Lacerda
Jun 7, 2016·Mutation Research. Genetic Toxicology and Environmental Mutagenesis·D Mourelatos
Jul 1, 2009·Nature Reviews. Nephrology·Vaibhav SahniZiauddin Ahmed
Dec 22, 2009·Dalton Transactions : an International Journal of Inorganic Chemistry·Luca Ronconi, Dolores Fregona
May 2, 2013·Bioconjugate Chemistry·Marya AhmedRavin Narain

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