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.

Diana, P., Martorana, A., Barraja, P., Montalbano, A., Carbone, A., Cirrincione G (2011). Nucleophilic substitutions in the isoindole series as a valuable tool to synthesize derivatives with antitumor activity. TETRAHEDRON, 67, 2072-2080.

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

DIANA, Patrizia;MARTORANA, Annamaria;BARRAJA, Paola;MONTALBANO, Alessandra;CARBONE, Anna;CIRRINCIONE, Girolamo
2011-01-01

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.
2011
Settore CHIM/08 - Chimica Farmaceutica
Diana, P., Martorana, A., Barraja, P., Montalbano, A., Carbone, A., Cirrincione G (2011). Nucleophilic substitutions in the isoindole series as a valuable tool to synthesize derivatives with antitumor activity. TETRAHEDRON, 67, 2072-2080.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/55071
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