Published in

Royal Society of Chemistry, Organic and Biomolecular Chemistry, 35(12), p. 6794-6799, 2014

DOI: 10.1039/c4ob00915k

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Orthogonal functionalisation of α-helix mimetics

This paper is available in a repository.
This paper is available in a repository.

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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.