Abstract
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 agents.
Keywords: Anticancer agent, HDAC inhibitor, Histone deacetylase (HDAC), Structure-activity relationship (SAR).
Mini-Reviews in Medicinal Chemistry
Title:Recent Progress in the Development of Histone Deacetylase Inhibitors as Anti-Cancer Agents
Volume: 13 Issue: 14
Author(s): Li Zhang, Jine Lei, Yuanyuan Shan, Hao Yang, Maxiaowei Song and Ying Ma
Affiliation:
Keywords: Anticancer agent, HDAC inhibitor, Histone deacetylase (HDAC), Structure-activity relationship (SAR).
Abstract: 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 agents.
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Cite this article as:
Zhang Li, Lei Jine, Shan Yuanyuan, Yang Hao, Song Maxiaowei and Ma Ying, Recent Progress in the Development of Histone Deacetylase Inhibitors as Anti-Cancer Agents, Mini-Reviews in Medicinal Chemistry 2013; 13 (14) . https://dx.doi.org/10.2174/13895575113136660102
DOI https://dx.doi.org/10.2174/13895575113136660102 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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