Orthogonal functionalisation of α-helix mimetics

Anna Barnard, Kérya Long, David J Yeo, Jennifer A Miles, Valeria Azzarito, George M Burslem, Panchami Prabhakaran, Thomas A Edwards, Andrew J Wilson
Organic & Biomolecular Chemistry 2014 September 21, 12 (35): 6794-9
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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