Macrocyclic Histone Deacetylase Inhibitors

Title: Macrocyclic Histone Deacetylase Inhibitors

Volume: 10 Issue: 14

Author(s): Sandra C. Mwakwari, Vishal Patil, William Guerrant and Adegboyega K. Oyelere

Affiliation:

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

Abstract: 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.

Cite this article as:

C. Mwakwari Sandra, Patil Vishal, Guerrant William and K. Oyelere Adegboyega, Macrocyclic Histone Deacetylase Inhibitors, Current Topics in Medicinal Chemistry 2010; 10 (14) . https://dx.doi.org/10.2174/156802610792232079