Novel histone deacetylase inhibitors bearing a 4-piperidin-4-yl-triazole scaffold as antitumor agents.

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ID: 57921
2019
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Abstract
Histone deacetylases have proven to be promising targets for the development of anticancer drugs. In this work, we reported the design and synthesis of a series of 20 novel hydroxamic acid-based histone deacetylase inhibitors with 4-piperidin-4-yl-triazole as the core structure. Five newly obtained compounds displayed excellent HDAC6 inhibitory activities. Among them, compounds WY-12 and WY-15 also exhibited excellent antiproliferative activities against six human tumor cell lines. WY-15 could increase the level of acetylated histone H3 in a dose-dependent manner. Furthermore, WY-15 remarkably induced cell cycle arrest of Sy5y cancer cells in G /G phase. Finally, the high potency of compound WY-15 toward HDAC6 was rationalized by molecular docking study.
Reference Key
wang2019noveldrug Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Yan Wang, Li Su, Qiang Wang, Li Zhang, Yepeng Luan
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Journal drug development research
Year 2019
DOI
10.1002/ddr.21603
URL
Keywords
Docking inhibitor antitumor histone deacetylase

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