2. Academic Validation
  3. Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors

Design, synthesis and activity evaluation of indole-based double - Branched HDAC1 inhibitors

  • Bioorg Med Chem. 2019 Apr 15;27(8):1595-1604. doi: 10.1016/j.bmc.2019.03.008.
Qiuqiong Zhang 1,  Jiahui Lv 1,  Feng He 1,  Chenggong Yu 1,  Ying Qu 1,  Xiangna Zhang 1,  Ana Xu 1,  Jingde Wu 2
Affiliations

Affiliations

  • 1 Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Science, Shandong University, 44 West Wenhua Road, 250012 Ji'nan, Shandong, PR China.
  • 2 Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Science, Shandong University, 44 West Wenhua Road, 250012 Ji'nan, Shandong, PR China. Electronic address: wujingde70@sdu.edu.cn.
PMID: 30879863 DOI: 10.1016/j.bmc.2019.03.008
Abstract

Histone deacetylases inhibitors (HDACIs) represents effective treatments for Cancer. In continuing our efforts to develop novel and potent HDACIs, a series of N-hydroxycinnamamide-based HDACIs with aromatic ring and various aliphatic linker have been successfully designed and synthesized. Biological evaluations established that compounds 4h, 4i, 4j, 4l, 4r showed superior inhibition on histone deacetylase and antiproliferative activity in some solid tumor cell lines [HeLa, SK-N-BE(2), PC-3] compared to the known inhibitor SAHA. Among these analogs, 4l exhibited selectivity to HDAC1.

Keywords

Antiproliferative activity; HDAC inhibitors; Molecular docking; Selectivity.

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