Syntheses and Biological Evaluation of Novel Hydroxamic Acid Derivatives Containing Purine Moiety as Histone Deacetylase Inhibitors

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  • Xu Zhaoxing
    School of Pharmaceutical Sciences, Nanchang University
  • Yang Yongchao
    School of Pharmaceutical Sciences, Nanchang University
  • Mai Xi
    School of Pharmaceutical Sciences, Nanchang University
  • Liu Bin
    School of Pharmaceutical Sciences, Nanchang University
  • Xiong Yuanzhen
    School of Pharmaceutical Sciences, Nanchang University
  • Feng Lihuang
    School of Pharmaceutical Sciences, Nanchang University
  • Liao Yijing
    School of Pharmaceutical Sciences, Nanchang University
  • Zhang Yu
    School of Pharmaceutical Sciences, Nanchang University
  • Wang Huanlu
    School of Pharmaceutical Sciences, Nanchang University
  • Ouyang Leiting
    School of Pharmaceutical Sciences, Nanchang University
  • Liu Shuhao
    School of Pharmaceutical Sciences, Nanchang University

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<p>The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, the most promising compound was 7m′. Western blot analysis indicated the compounds 7f′, 7l′, 7m′, 7o′ could increase histone H3 acetylation levels in HCT116 and K562 cell lines, and 7m′ increased the level of acetyl histone H3 in a dose-dependent manner, which is similar to the behavior of suberoylanilide hydroxamic acid (SAHA). Molecular docking study revealed that the conformation of 7m′ in the active site of HDAC2 was similar to positive drug SAHA, which were oriented with the hydroxamic acid towards the catalytic center and formed metal binding with zinc ion.</p>

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