Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.

Abstract

Inhibitors of histone deacetylases (HDAC) are emerging as a promising class of anti-cancer agents. A mercaptoamide functionality was designed as a bidentate zinc chelator and incorporated into the hydroxamic acid based SAHA (1) scaffold in order to identify non-hydroxamate compounds as potential inhibitors of histone deacetylases. Two sets of mercaptoamides 2 and 3 with varying spacer length were synthesized and their HDAC inhibitory activity was evaluated. Low micromolar inhibition was observed for mercaptoamides 2e, 3b, and 3d.

• Authors: Sampath-Kumar Anandan, John S Ward, Richard D Brokx, Mark R Bray, Dinesh V Patel, Xiao-Xi Xiao
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 15 Issue 8 Pg. 1969-72 (Apr 15 2005) ISSN: 0960-894X [Print] England
• PMID: 15808449 (Publication Type: Journal Article)

Chemical References

• Amides
• Enzyme Inhibitors
• Histone Deacetylase Inhibitors
• Hydroxamic Acids
• Sulfhydryl Compounds

Topics

• Amides (chemistry)
• Enzyme Inhibitors (chemistry, classification, pharmacology)
• Histone Deacetylase Inhibitors
• Hydroxamic Acids (chemistry)
• Sulfhydryl Compounds (chemistry)