Largazole is a selective anticancer agent isolated form a marine organism.  It is a histone deacetylase (HDAC) inhibitor and can be used for epigenetic regulation of gene expression to develop anticancer drugs. HDAC inhibitors currently in clinical use suffer from undesirable side effects as they lack isoform selectivity. Isoform selective HDAC inhibitors are being developed to reduce these undesirable side effects. The depsipeptide ring of largazole interacts with the less conserved hydrophobic rim of the HDAC active site and can be targeted for developing isoform selective HDAC inhibitors. We have designed and synthesized largazole analogues by structurally altering its depsipeptide ring. The synthesis and biological activity of these novel largazole analogues will be presented.

Largazole analogs as selective histone deacetylase inhibitors

248th National Meeting (2014)

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