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Medicinal Chemistry Insights into Novel HDAC Inhibitors: An Updated Patent Review (2012-2016)

[ Vol. 12 , Issue. 1 ]


Peng Zhan, Xueshun Wang, Xinyong Liu and Takayoshi Suzuki   Pages 16 - 34 ( 19 )


Background: Many laboratories have made intensive efforts to develop potent, selective, and orally bioavailable HDAC inhibitors (HDACIs). Novel HDACIs are being developed with the objective of improving potency and selectivity against specific types of cancers or non-cancer diseases.

Objective: This updated patent review is an attempt to compile the work of various researchers of HDACIs from 2012 to mid 2016, and to enlighten and surprise both newcomers in this field and devoted medicinal chemists.

Method: According to the literature research and the writers' own research experience in the discovery of HDAC inhibitors.

Results: The inhibitors possessing new chemical scaffolds have attracted immense interest because they have the ability to improve HDAC isoform specificity and pharmaceutical properties. Focus is given to emerging medicinal chemistry principles and insights into the discovery and development of HDAC inhibitors.

Conclusion: The development of effective HDACIs is shifting from trial-and-error approaches to sophisticated strategies. Effective profiling technologies will continue to have important utility.


Chelating, drug design, epigenetics, HDAC inhibitor, histone acetylation, metalloprotein, patent, synthesis.


CREST, Japan Science and Technology Agency (JST), 4-1-8 Honcho, Kawaguchi, Saitama 332-0012

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