Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction

The design, synthesis and evaluation of 24 isoindolinones as potential inhibitors of the MDM2-p53 interaction is described. The most potent inhibitor NU8231 (ELISA: IC50 = 5.3 ± 0.9 μM) displays cellular activity in human SJSA cells.