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Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes
Authors:D'Errico Stefano  Oliviero Giorgia  Piccialli Vincenzo  Amato Jussara  Borbone Nicola  D'Atri Valentina  D'Alessio Francesca  Di Noto Rosa  Ruffo Francesco  Salvatore Francesco  Piccialli Gennaro
Affiliation:Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Napoli, Italy. stefano.derrico@unina.it
Abstract:
Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay.
Keywords:Dinuclear platinum complexes   Nucleosides   Solid-phase synthesis   Anti-tumor compounds
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