Abstract

AbstractSyntheses of novel 16‐membered macrocyclic peptidomimetics are reported, which employ iterative peptide coupling followed by high yielding ring‐closing metathesis (RCM) as the key cyclization step. The target macrocyclic compounds include examples containing a (2S)‐amino‐8‐oxodecanoic acid (Aoda) residue as analogues of apicidin A, a known potent histone deacetylase (HDAC) inhibitor. These showed modest levels of biological activity as HDAC inhibitors.

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