Design, synthesis and biological evaluation of the novel isoindolinone derivatives

Jiang Liu, Luyao Wang, Na Guo*

Abstract

Isoindolinones have a wide range of biological activities, such as antitumor, anticonvulsant and so on. Some isoindolinone derivatives have been studied as antitumor drug molecules. In this paper, we would like to report the design, synthesis and biological activities of a series of novel 2-benzyl-6-substituted-ethoxy-isoindolinone derivatives which have not been reported yet. All the target compounds (9-12) were characterized by 1H NMR and ESI-MS and were tested for their cytotoxicity using HT-29, K562, HepG2 cell line. Preliminary result showed that tert-butyl 4-(2-(2-benzyl-3-oxoisoindolin-5-yloxy) ethyl) piperazine-1-carboxylate (11) demonstrated antitumor activity against HepG2 cancer cell with an IC50 of 5.89 μM .