Structure-Activity Relationships within a Series of [sigma]1 and [sigma]2 Receptor Ligands: Identification of a [sigma]2 Receptor Agonist (BS148) with Selective Toxicity against Metastatic Melanoma

A new series of spirocyclic σ receptor (σR) ligands were prepared and studied. Most were found to have a high affinity and selectivity for σ1R; three compounds were shown to be σ1R agonists, while another proved to be the only σ1R antagonist. Only one of the σ1R agonists (BS148) also exhibited σ2R s...

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Veröffentlicht in:	ChemMedChem 2017-11, Vol.12 (22), p.1893
Hauptverfasser:	Franchini, Silvia, Sorbi, Claudia, Battisti, Umberto Maria, Tait, Annalisa, Bencheva, Leda Ivanova, Cichero, Elena, Fossa, Paola, Cilia, Antonio, Prezzavento, Orazio, Ronsisvalle, Simone, Arico, Giuseppina, Benassi, Luisa, Vaschieri, Cristina, Azzoni, Paola, Magnoni, Cristina, Brasili, Livio
Format:	Artikel
Sprache:	eng
Schlagworte:	Apoptosis Cell death Cell lines Ligands Melanocytes Melanoma Metastases Metastasis Selectivity Skin cancer Structure-activity relationships Toxicity
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