2. Academic Validation
  3. Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors

Design, synthesis and biological evaluation of 4-piperazinyl-containing Chidamide derivatives as HDACs inhibitors

  • Bioorg Med Chem Lett. 2017 Jul 15;27(14):3162-3166. doi: 10.1016/j.bmcl.2017.05.026.
Qingwei Zhang 1,  Bingliu Lu 1,  Jianqi Li 2
Affiliations

Affiliations

  • 1 Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 201203, China; Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai 201203, China.
  • 2 Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 201203, China; Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai 201203, China. Electronic address: sipiqingwei@163.com.
PMID: 28532668 DOI: 10.1016/j.bmcl.2017.05.026
Abstract

The synthesis and biological evaluation of a variety of 4-piperazinyl-containing Chidamide derivatives is described. Some of these compounds were shown to inhibit HDAC1 with IC50 values below micromolar range, and inhibited proliferation of several human Cancer cells, not possessing toxicity to human normal cells and hERG K+ ion channels. Compound 9g, proved to be the most potent and efficacious derivative in this series, was orally active in an HCT116 xenograft model in vivo.

Keywords

Anticancer activity; Chidamide derivatives; HDACs inhibitors; Molecular docking.

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