Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes

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.

Graphical abstractThree novel nucleoside-tethered dinuclear platinum(II) complexes were synthesised through a solid-phase strategy. One complex proved to be more cytotoxic than cisplatin against MCF7 cancer cell line in a short-term exposure assay.Figure optionsDownload full-size imageDownload as PowerPoint slide