Highlights•We highlight recent development of small-molecule α-helix mimetics.•We review
solid-phase synthesis of small-molecule α-helix mimetics.•We highlight HTS methods for the …

α-Helices play a critical role in mediating many protein–protein interactions (PPIs) as
recognition motifs. Therefore, there is a considerable interest in developing small molecules …

Many biologically active α-helical peptides adopt amphiphilic helical structures that contain
hydrophobic residues on one side and hydrophilic residues on the other side. Therefore, α …

Small molecules mimicking α-helices are of great interest since numerous protein− protein
interactions use helical structures at the interface. With a goal of generating libraries of α …

Herein, we report a strategy for generating conformationally restricted α-helix mimetic small
molecules by introducing covalent bridges that limit rotation about the central axis of α-helix …

Proteins in nature fold into native conformations in which combinations of peripherally
projected aliphatic, aromatic and ionic functionalities direct a wide range of properties. α …

Protein–protein interactions play critical roles in a wide variety of biological processes, and
their dysregulations contribute to the pathogenesis of several diseases, including cancer …

The design and synthesis of small molecule α-helix mimetics has been a productive field
over the past decade. These compounds have performed well in a variety of biological …

The synthesis of an amphiphilic, nonpeptidic scaffold that mimics the presentation of i, i+ 4,
and i+ 7 residues of an α-helix is presented. The approach uses a pyridazine core, and …

Stabilized α-helices and nonpeptidic helix mimetics have emerged as powerful molecular
scaffolds for the discovery of protein–protein interaction inhibitors. Protein-protein …