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Issue 12, 2014
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Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors

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Abstract

Histone deacetylase (HDAC) is a clinically validated target for anti-tumor therapy. In order to increase HDAC inhibition and efficiency, we developed a series of novel substituted purine hydroxamic acids as potent HDAC inhibitors. The biological evaluation suggests that compound 5r (IC50 = 0.075 μmol L−1) exhibits better HDAC1 and 2 inhibitory activity compared to the approved drug SAHA (IC50 = 0.14 μmol L−1). Further biological evaluation indicated that compounds 5r, 5w, and 5x have potent anti-proliferative activities against eight tumor cells, including MDA-MB231, KG1, PC3, U937 and so on.

Graphical abstract: Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors

  • This article is part of the themed collection: Epigenetics
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Publication details

The article was received on 08 May 2014, accepted on 14 Sep 2014 and first published on 15 Sep 2014


Article type: Concise Article
DOI: 10.1039/C4MD00203B
Citation: Med. Chem. Commun., 2014,5, 1887-1891

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    Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors

    J. Wang, F. Sun, L. Han, X. Hou, X. Pan, R. Liu, W. Tang and H. Fang, Med. Chem. Commun., 2014, 5, 1887
    DOI: 10.1039/C4MD00203B

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