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

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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.
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wang2019noveldrug Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Wang, Yan;Su, Li;Wang, Qiang;Zhang, Li;Luan, Yepeng;
Journal drug development research
Year 2019
DOI
10.1002/ddr.21603
URL
Keywords
Docking inhibitor antitumor histone deacetylase

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