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Histone deacetylases are able to catalyze the hydrolysis of N-acetyl lysine residues of histones which package chromosomal DNA. Therefore they play an important role in mediating gene expression and cell proliferation. HDAC inhibitors have not only shown promise as antiparasitic, antineurodegenerative, antirheumatologic agents and immunosuppressant, but as potent anticancer agents by inducing cell cycle arrest, differentiation and apoptosis. This review highlights recent development in design, synthesis and biological evaluation of HDAC inhibitors for cancer therapy.