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: http://hdl.handle.net/10447/55071
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.