2. Academic Validation
  3. Synthesis and bioactivity evaluation of 2,3-diaryl acrylonitrile derivatives as potential anticancer agents

Synthesis and bioactivity evaluation of 2,3-diaryl acrylonitrile derivatives as potential anticancer agents

  • Bioorg Med Chem Lett. 2017 Jan 1;27(1):81-85. doi: 10.1016/j.bmcl.2016.11.025.
Jun Ma 1,  Jiajun Li 1,  Yu-Shun Tian 2
Affiliations

Affiliations

  • 1 Yanbian University, College of Pharmacy, Yanji City, Jinlin Province 133002, PR China.
  • 2 Yanbian University, College of Pharmacy, Yanji City, Jinlin Province 133002, PR China. Electronic address: tyshhanguo@hanmail.net.
PMID: 27887843 DOI: 10.1016/j.bmcl.2016.11.025
Abstract

Thirty novel derivatives of 2,3-diaryl acrylonitrile were synthesized and evaluated for biological activity. Preliminary investigations of antitumor activity in vitro showed that most of the synthesized compounds have significant antiproliferative effects on human Cancer cell lines, such as BEL-7402, HeLa, and HCT116 with IC50 values in the range of 0.13-60.23μM without significant toxic effects on the non-cancerous human liver cell line L-02. In particular, compounds 4d and 4p were found to be the most potent against HeLa (4.20μM) and HCT116 cells (0.13μM), respectively, with superior or similar in vitro efficacy to that of the broad-spectrum Anticancer drug taxol.

Keywords

2,3-Diaryl acrylonitrile; Antitumor activity; Cyano group; Migration; Selective inhibition.

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