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  • Title: Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.
    Author: Liu R, Wang J, Tang W, Fang H.
    Journal: Bioorg Med Chem; 2016 Apr 01; 24(7):1446-54. PubMed ID: 26907204.
    Abstract:
    Histone deacetylase inhibitors have been proved to be great potential for the treatment of cancer. Recently, we designed and modified a series of substituted purine hydroxamate analogs as potent HDAC inhibitors based on our previous studies. The target compounds were investigated for their in vitro HDAC inhibitory activities and anti-proliferative activities. Results indicated that these compounds could effectively inhibit HDAC and possess obvious anti-proliferative activity against tumor cells. Promisingly, target compounds 4m and 4n outperformed SAHA in both enzymatic inhibitory activity and cellular anti-proliferative activity assay.
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