Three novel inosine-based dinuclear Pt complexes were synthesized via a solid-phase strategy. In these compds., 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 Pt along with a chloride. The synthesized 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.
Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes / D'Errico, Stefano; Oliviero, Giorgia; Piccialli, Vincenzo; Amato, Jussara; Borbone, Nicola; D'Atri, Valentina; D'Alessio, F; DI NOTO, Rosa; Ruffo, Francesco; Salvatore, Francesco; Piccialli, Gennaro. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 21:19(2011), pp. 5835-5838. [10.1016/j.bmcl.2011.07.104]
Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes
D'ERRICO, STEFANO;OLIVIERO, GIORGIA;PICCIALLI, VINCENZO;AMATO, JUSSARA;BORBONE, NICOLA;D'ATRI, VALENTINA;DI NOTO, ROSA;RUFFO, FRANCESCO;SALVATORE, FRANCESCO;PICCIALLI, GENNARO
2011
Abstract
Three novel inosine-based dinuclear Pt complexes were synthesized via a solid-phase strategy. In these compds., 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 Pt along with a chloride. The synthesized 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
