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Nucleophilic substitutions in the isoindole series as a valuable tool to synthesize derivatives with antitumor activity

  • Autori: Diana, P.; Martorana, A.; Barraja, P.; Montalbano, A.; Carbone, A.; Cirrincione, G.
  • Anno di pubblicazione: 2011
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • Parole Chiave: Isoindoles Nucleophilic substitutions; Antitumor activity; Docking; Colchicine analogues;
  • OA Link:


A novel synthetic approach to the synthesis of 3-substituted isoindoles through nucleophilic substitution of 3-halo derivatives by charged carbon, and neutral nitrogen, oxygen, and sulfur nucleophiles, assisted by a 1-acyl group, is reported. Aryl-thio-isoindoles, obtained through a direct nucleophilic substitution with sulfur nucleophiles, showed cytotoxic activity, with GI50 values from micromolar to sub-micromolar concentrations, against the total number of cell lines investigated.