Nucleophilic substitutions in the isoindole series as a valuable tool to synthesize derivatives with antitumor activity
2011
Diana, Patrizia | Martorana, Annamaria | Barraja, Paola | Montalbano, Alessandra | Carbone, Anna | Cirrincione, Girolamo
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.
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