Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents

Journal of Enzyme Inhibition and Medicinal Chemistry
Ya-Bing XinYu-Shun Tian

Abstract

To identify anticancer agents with high potency and low toxicity, a series of (Z)-styrylbenzene derivatives were synthesised and evaluated for anticancer activities using a panel of nine cancer cell lines and two noncancerous cell lines. Most derivatives exhibited significant anti-proliferative activities against five cancer cell lines, including MGC-803 and BEL-7402. (Z)-3-(p-Tolyl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile (6h) showed a strong inhibitory effect on MGC-803 cells (IC50 < 0.01 µM) and exhibited stronger anti-proliferative activity than taxol (IC50 < 0.06 ± 0.01 µM). The IC50 value of 6h in L-02 cells was 10,000-fold higher than in MGC-803 cells. Compound 6h inhibited proliferation of BEL-7402 cells by arresting at the G2/M phase through up-regulation of cyclin B1 expression, down-regulation of cyclin A and D1 expression, and induction of apoptosis. In addition, 6h inhibited the migration of BEL-7402 cells and the formation of cell colonies.

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Dec 13, 2017·Journal of Enzyme Inhibition and Medicinal Chemistry·Hong-Jian ZhangZhe-Shan Quan

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Citations

Aug 14, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Jia LiuPing Wang

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Methods Mentioned

BETA
flow cytometry

Software Mentioned

AutoDockTools
Chem
Cell Quest
Discovery Studio
ModFit LT

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