Syntheses and Biological Activity of the HDAC Class I Inhibitor Largazole

Abstract

Histone deacetylase inhibitors are an emerging class of antiproliferative agents that have the potential to combat cancer on an epigenetic level. The recently reported marine natural product largazole has been recently isolated in trace amounts from cyanobacteria and displays a very potent and selective antiproliferative activity towards a number of cell lines. Several lines of evidence suggested it might act as a histone deacetylase inhibitor. These compelling properties have generated considerable interest in the synthetic community which resulted in several total syntheses of largazole. The present review offers a brief overview of the synthetic routes and some early structure–activity relationships.