Nucleophilic substitutions in the isoindole series as a valuable tool to synthesize derivatives with antitumor activity
- Authors: Diana, P; Martorana, A; Barraja, P; Montalbano, A; Carbone, A; Cirrincione G
- Publication year: 2011
- Type: Articolo in rivista (Articolo in rivista)
- Key words: Isoindoles Nucleophilic substitutions; Antitumor activity; Docking; Colchicine analogues;
- OA Link: http://hdl.handle.net/10447/55071
Abstract
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.