Drug Discov Ther. 2008;2(4):211-215.

Novel N-hydroxybenzamide histone deacetylase inhibitors as potential anti-cancer agents.

Jiao J, Fang H, Xu WF

Histone deacetylases (HDACs) are a class of Zn²⁺ dependent metalloproteases that play an important role in tumorigenesis. Inhibition of HDACs may be a potential strategy for cancer therapy. This study designed and synthesized a series of novel N-hydroxybenzamide histone deacetylase inhibitors based on the structural features of suberoylanilide hydroxamic acid (SAHA), the first HDAC inhibitor that came to market. Preliminary biological evaluation in vitro found that most of the inhibitors had satisfactory inhibitory activity (IC₅₀ =1-17 μM) against HDACs and HCT116 tumor cells.

Full Text: