Orthogonal functionalisation of α-helix mimetics.

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Barnard, A ; Long, K ; Yeo, DJ ; Miles, JA ; Azzarito, V ; Burslem, GM ; Prabhakaran, P ; Edwards, TA ; Wilson, AJ (2014)
  • Publisher: Royal Society of Chemistry

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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