Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents
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 acti...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2018-01-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/14756366.2018.1513925 |
| _version_ | 1818154894618525696 |
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| author | Ya-Bing Xin Jia-Jun Li Hong-Jian Zhang Jun Ma Xin Liu Guo-Hua Gong Yu-Shun Tian |
| author_facet | Ya-Bing Xin Jia-Jun Li Hong-Jian Zhang Jun Ma Xin Liu Guo-Hua Gong Yu-Shun Tian |
| author_sort | Ya-Bing Xin |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-11T14:33:46Z |
| format | Article |
| id | doaj.art-e620989c8d2e4fa4b1711de2aead7375 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-12-11T14:33:46Z |
| publishDate | 2018-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-e620989c8d2e4fa4b1711de2aead73752022-12-22T01:02:18ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742018-01-013311554156410.1080/14756366.2018.15139251513925Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agentsYa-Bing Xin0Jia-Jun Li1Hong-Jian Zhang2Jun Ma3Xin Liu4Guo-Hua Gong5Yu-Shun Tian6Yanbian UniversityYanbian UniversityYanbian UniversityJiangsu Hansoh Pharmaceutical Group Co., LtdYanbian UniversityFirst Clinical Medical College of Inner Mongolia University for NationalitiesYanbian UniversityTo 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.http://dx.doi.org/10.1080/14756366.2018.1513925Styrylbenzenecyanoselective toxic effectanticancersynthesis |
| spellingShingle | Ya-Bing Xin Jia-Jun Li Hong-Jian Zhang Jun Ma Xin Liu Guo-Hua Gong Yu-Shun Tian Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents Journal of Enzyme Inhibition and Medicinal Chemistry Styrylbenzene cyano selective toxic effect anticancer synthesis |
| title | Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents |
| title_full | Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents |
| title_fullStr | Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents |
| title_full_unstemmed | Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents |
| title_short | Synthesis and characterisation of (Z)-styrylbenzene derivatives as potential selective anticancer agents |
| title_sort | synthesis and characterisation of z styrylbenzene derivatives as potential selective anticancer agents |
| topic | Styrylbenzene cyano selective toxic effect anticancer synthesis |
| url | http://dx.doi.org/10.1080/14756366.2018.1513925 |
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