Aromatic oligoamide foldamers with a 'wet edge' as inhibitors of the α-helix-mediated p53-hDM2 protein-protein interaction

摘要

This paper describes the design, synthesis and structural analysis of a 3-O-alkylated aromatic oligoamide that incorporates an additional hydrophilic 6-O-alkyl substituent in the central monomer. This oligomer exhibits low μM inhibitory potency against the p53-hDM2 interaction compared with its unfunctionalised counterpart and significantly improved solubility.