Histone deacetylases (HDACs) regulate the expression and activity of many proteins in both cancer initiation
and cancer progression. HDACs are now recognized as promising targets for anticancer agent development. HDAC
inhibitors (HDACIs) are emerging as promising anticancer drugs which possess tumor-selective cytotoxicity. HDACIs
could promote growth arrest, differentiation, and apoptosis of cancer cells, with minimal effects on normal tissue.
Research of HDACIs is now becoming an interesting field. HDACIs comprise structurally diverse anticancer agents and
have been widely used in the clinic. This review describes recent progress in the development of HDACIs, especially
focusing on the design strategies, novel chemical structures, biological properties and structure-activity relationships
(SARs) of HDACIs. We hope it will be helpful for medicinal chemists who are interested in the discovery of anticancer
Keywords: Anticancer agent, HDAC inhibitor, Histone deacetylase (HDAC), Structure-activity relationship (SAR).
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