2. Academic Validation
  3. Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity

Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity

  • Bioorg Med Chem. 2015 Aug 1;23(15):4481-4488. doi: 10.1016/j.bmc.2015.06.015.
Wenwen Duan 1,  Jinning Hou 1,  Xiaojing Chu 2,  Xiaoqian Li 3,  Jian Zhang 4,  Jin Li 1,  Wenfang Xu 1,  Yingjie Zhang 5
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, People's Republic of China.
  • 2 Weifang Bochuang International Biological Medicinal Institute, Weifang, Shandong 261061, People's Republic of China.
  • 3 Color Ultrasonic Room, The People's Hospital of Shouguang, Weifang, Shandong 262700, People's Republic of China.
  • 4 Department of Medical Chemistry, School of Pharmacy, Weifang Medical University, West Baotong Street, Weifang, Shandong 261053, People's Republic of China.
  • 5 Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, People's Republic of China. Electronic address: zhangyingjie@sdu.edu.cn.
PMID: 26122774 DOI: 10.1016/j.bmc.2015.06.015
Abstract

A novel series of histone deacetylases inhibitors (HDACIs) containing benzofuroxan pharmacophore as nitric oxide (NO) donor were designed based on the combination principle and 'multifunctional drugs' theory. As a novel study on embedding NO donor into the structure of HDACIs, all designed hybrid compounds, especially 19d and 24d, displayed remarkable HDACs inhibitory activity and outstanding antiproliferative activity on tumor cells. Besides, they could produce high levels of NO in HCT-116 cells; furthermore, their antiproliferative activity on HCT-116 cells could be diminished by pretreatment with hemoglobin, as the NO scavenger, in a dose-dependent manner. All in all, our designed compounds displayed great inhibitory activities and might offer a prospective avenue to discover novel anti-cancer drugs.

Keywords

Benzofuroxan; Epigenetic; HDAC inhibitor; Multifunctional drugs; Nitric oxide.

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