Orthogonal functionalisation of α-helix mimetics
2014
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.
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