2. Academic Validation
  3. Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors

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

  • Bioorg Med Chem. 2015 Aug 1;23(15):4364-4374. doi: 10.1016/j.bmc.2015.06.024.
Lei Wang 1,  Xuben Hou 1,  Huansheng Fu 1,  Xiaole Pan 1,  Wenfang Xu 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, Ji'nan, Shandong 250012, PR China.
  • 2 School of Pharmacy, University of Wisconsin, 777 Highland Avenue, Madison 53705, USA.
  • 3 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China. Electronic address: haofangcn@sdu.edu.cn.
PMID: 26149591 DOI: 10.1016/j.bmc.2015.06.024
Abstract

Inhibition of HDACs activity has become a promising therapeutic strategy in clinical practice to reverse the abnormal epigenetic states of Cancer and Other Diseases. Therefore, HDAC inhibitors become a relatively new class of anti-cancer agent. In the present study, we reported the design and synthesis of a series of novel HDAC inhibitors using various substituted quinoline rings as the cap group. In vitro studies showed that some compounds have good inhibitory activities against HDACs and potent antiproliferative activities in some tumor cell lines. Especially, compound 9w (IC50=85 nM), exhibited better inhibitory effect compared with SAHA (IC50=161 nM).

Keywords

Anti-proliferative; HDAC; Hydroxamic acid; Inhibitor; Quinoline.

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