%0 Journal Article
%T Design and synthesis of novel histone deacetylase 6 inhibitors with benzyl-triazole as the core skeleton.
%A Gao JJ
%A Luan YP
%A Miao H
%A Mou ZS
%A Su L
%A Wang BL
%A Zhang L
%J BioScienceTrends
%D 2019
%R BioScience Trends. 2019 ;13(3):267-272. (DOI: 10.5582/bst.2019.01054)
%X SUMMARY: In the field of epigenetics, histone deacetylases (HDACs) are important members and well validated targets for anti-cancer drugs discovery. In this study, we designed and synthesized twenty-seven novel hydroxamic acid-based HDAC inhibitors (HDACis) with benzyl-triazole as the core skeleton. Most target compounds displayed excellent inhibition rates toward HDACs. Among them, compounds ZM-22 to ZM-27 with inhibition rates more than 90% toward HDACs exhibited potent inhibitory activity toward HDAC6, and ZM-23 possessed the best selectivity to HDAC6 over HDAC1. The high potency of compound ZM-23 toward HDAC6 was rationalized by molecular docking simulation. This series of compounds is worthy for further anti-cancer activity evaluation and structural optimization works. Key Words: Histone deacetylase, isoform, selective, inhibitor, anti-tumor Full Text: PDF(538KB
%U http://www.biosciencetrends.com/getabstract.php?id=1746