oligobenzamides

These mimetics exhibit highest affinity for MDM2 and the best selectivity when binding between MMD2 and BCL-2 family proteins was compared.[ 380 ] Notably, these compounds also proved to be active in cell-based assays.[ 381 ] Cell-permeable pyrrolopyrimidines ( 30 ) were also used to disrupt both the p53–MDM2 and the p53–MDMX complexes, thereby promoting p53-dependent apoptosis in cultured cancer cells.[ 288 ] Although less potent, hydrogen-bond-guided 3-O-alkylated ( 32 ),[ 297, 382 ] 2-O-alkylated ( 33 ),[ 293 ] and N-alkylated oligobenzamides ( 34 )[ 294, 298, 299 ] as well as hybrids[ 300 ] inhibit the p53–HMD2 complex in vitro.

2015 June 26, Marta Pelay-Gimeno et al., “Structure-Based Design of Inhibitors of Protein–Protein Interactions: Mimicking Peptide Binding Epitopes”, in Angewandte Chemie (International Ed. in English), volume 54, →DOI