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Macrocyclic Histone Deacetylase Inhibitors

[ Vol. 10 , Issue. 14 ]


Sandra C. Mwakwari, Vishal Patil, William Guerrant and Adegboyega K. Oyelere   Pages 1423 - 1440 ( 18 )


Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, antineurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have been reported including aryl hydroxamates, benzamides, short-chain fatty acids, electrophilic ketones, and macrocyclic peptides. Macrocyclic HDACi possess the most complex cap-groups which interact with HDAC enzyme's outer rim and have demonstrated excellent HDAC inhibition potency and isoform selectivity. This review focuses on the recent progress and current state of macrocyclic HDACi.


Cyclic tetrapeptide, depsipeptide, peptide mimetic, macrolide, ketolide, macrocycles, histone deacetylase inhibitors, HDAC


School of Chemistry and Biochemistry, Parker H. Petit Institute of Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400.

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