Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes
| Autor: | Francesco Salvatore, Francesca D'Alessio, Jussara Amato, Francesco Ruffo, Nicola Borbone, Stefano D'Errico, Valentina D'Atri, Giorgia Oliviero, Gennaro Piccialli, Rosa Di Noto, Vincenzo Piccialli |
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| Přispěvatelé: | 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 |
| Rok vydání: | 2011 |
| Předmět: |
Antimetabolites
Antineoplastic Stereochemistry Clinical Biochemistry Pharmaceutical Science chemistry.chemical_element Antineoplastic Agents Ethylenediamine nucleoside Diamines Biochemistry Dinuclear platinum complexe Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Solid-phase synthesis Hexylamine Cell Line Tumor Diamine Drug Discovery Tumor Cells Cultured medicine Humans Inosine Molecular Biology Solid-Phase Synthesis Techniques Solid-phase synthesi Aged Platinum Molecular Structure Chemistry Organic Chemistry Nucleosides antitumor compounds Drug Design Molecular Medicine Female Amine gas treating Drug Screening Assays Antitumor Nucleoside HeLa Cells medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:5835-5838 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.07.104 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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