3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents
A series of cis-restricted 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines as novel tubulin polymerisation inhibitors was designed based on molecular docking. Compound 9p, exhibited potent antiproliferative activity against HeLa, MCF-7, and A549 cell lines. Mechanism studies indicated that 9p potently in...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2024-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2023.2286939 |
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| _version_ | 1846107544418779136 |
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| author | Chao Wang Yujing Zhang Shanbo Yang Lingyu Shi Yutao Xiu Yudong Wu Hongfei Jiang |
| author_facet | Chao Wang Yujing Zhang Shanbo Yang Lingyu Shi Yutao Xiu Yudong Wu Hongfei Jiang |
| author_sort | Chao Wang |
| collection | DOAJ |
| description | A series of cis-restricted 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines as novel tubulin polymerisation inhibitors was designed based on molecular docking. Compound 9p, exhibited potent antiproliferative activity against HeLa, MCF-7, and A549 cell lines. Mechanism studies indicated that 9p potently inhibited tubulin polymerisation and disrupted the microtubule dynamics of tubulin in HeLa cells. Moreover, 9p could cause G2/M phase cell cycle arrest and apoptosis in HeLa cells. In addition, the prediction of physicochemical properties disclosed that 9p conformed well to the Lipinski’s rule of five. The initial results suggest that the 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines could serve as a promising scaffold for the development of novel anticancer drugs. |
| format | Article |
| id | doaj-art-20346a9d73e8457f95d03cd1b57f851a |
| institution | Kabale University |
| issn | 1475-6366 1475-6374 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj-art-20346a9d73e8457f95d03cd1b57f851a2024-12-26T09:30:43ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742024-12-0139110.1080/14756366.2023.22869393-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agentsChao Wang0Yujing Zhang1Shanbo Yang2Lingyu Shi3Yutao Xiu4Yudong Wu5Hongfei Jiang6Cancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaThe Affiliated Cardiovascular Hospital of Qingdao University, Qingdao University, Qingdao, ChinaCancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaCancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaCancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaCancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaCancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, ChinaA series of cis-restricted 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines as novel tubulin polymerisation inhibitors was designed based on molecular docking. Compound 9p, exhibited potent antiproliferative activity against HeLa, MCF-7, and A549 cell lines. Mechanism studies indicated that 9p potently inhibited tubulin polymerisation and disrupted the microtubule dynamics of tubulin in HeLa cells. Moreover, 9p could cause G2/M phase cell cycle arrest and apoptosis in HeLa cells. In addition, the prediction of physicochemical properties disclosed that 9p conformed well to the Lipinski’s rule of five. The initial results suggest that the 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines could serve as a promising scaffold for the development of novel anticancer drugs.https://www.tandfonline.com/doi/10.1080/14756366.2023.2286939Combretastatin A-4antiproliferative activitypyridinetubulinmolecular docking |
| spellingShingle | Chao Wang Yujing Zhang Shanbo Yang Lingyu Shi Yutao Xiu Yudong Wu Hongfei Jiang 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents Journal of Enzyme Inhibition and Medicinal Chemistry Combretastatin A-4 antiproliferative activity pyridine tubulin molecular docking |
| title | 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents |
| title_full | 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents |
| title_fullStr | 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents |
| title_full_unstemmed | 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents |
| title_short | 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents |
| title_sort | 3 aryl 4 3 4 5 trimethoxyphenyl pyridines inhibit tubulin polymerisation and act as anticancer agents |
| topic | Combretastatin A-4 antiproliferative activity pyridine tubulin molecular docking |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2023.2286939 |
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