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Histone deacetylase (HDAC) inhibition is a recent, clinically validated therapeutic strategy for cancer treatment.HDAC inhibitors hold great promise in cancer therapy due to their demonstrated ability to arrest proliferation of nearly all transformed cell types.However, most of these agents are non-selective inhibitors of all HDAC isoforms; and a large number of the identified HDAC inhibitors have not progressed beyond preclinical characterizations.Of the several structurally distinct small molecule HDACi reported, macrocyclic depsipeptides have the most complex recognition cap-group moieties and present an excellent opportunity for the modulation of the biological activities of HDAC inhibitors.Unfortunately, the structure-activity relationship (SAR) studies for this class of compounds have been impaired largely because most macrocyclic HDAC inhibitors known to date comprise of complex peptide macrocycles.