2. Academic Validation
  3. Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors

Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors

  • Bioorg Med Chem. 2016 Apr 1;24(7):1446-54. doi: 10.1016/j.bmc.2016.02.005.
Renshuai Liu 1,  Junhua Wang 1,  Weiping Tang 2,  Hao Fang 3
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Road, Ji'nan, Shandong 250012, PR China.
  • 2 School of Pharmacy, University of Wisconsin-Madison, Madison 53705, USA.
  • 3 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, 44 West Wenhua Road, Ji'nan, Shandong 250012, PR China. Electronic address: haofangcn@sdu.edu.cn.
PMID: 26907204 DOI: 10.1016/j.bmc.2016.02.005
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.

Keywords

Anticancer; Histone deacetylase; Inhibitor; Purine.

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