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Updated: Mar 11, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and bioactivity evaluation of 2,3-diaryl acrylonitrile derivatives as potential anticancer agents
Jun Ma1, Jiajun Li1, Yu-Shun Tian1
1Yanbian University, College of Pharmacy, Yanji City, Jinlin Province 133002, PR China.
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.
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