Orthogonal functionalisation of α-helix mimetics?

Organic & Biomolecular Chemistry Pub Date: 2014-07-28 DOI: 10.1039/C4OB00915K

Abstract

α-Helix mediated protein–protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using ‘click’ chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.

Graphical abstract: Orthogonal functionalisation of α-helix mimetics
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