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.File | Dimensione | Formato | |
---|---|---|---|
T2011,67,2072.pdf
Solo gestori archvio
Dimensione
451.84 kB
Formato
Adobe PDF
|
451.84 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.