3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents

AbstractA 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 pot...

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Main Authors: Chao Wang (Author), Yujing Zhang (Author), Shanbo Yang (Author), Lingyu Shi (Author), Yutao Xiu (Author), Yudong Wu (Author), Hongfei Jiang (Author)
Format: Book
Published: Taylor & Francis Group, 2024-12-01T00:00:00Z.
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001 doaj_20346a9d73e8457f95d03cd1b57f851a
042 |a dc 
100 1 0 |a Chao Wang  |e author 
700 1 0 |a Yujing Zhang  |e author 
700 1 0 |a Shanbo Yang  |e author 
700 1 0 |a Lingyu Shi  |e author 
700 1 0 |a Yutao Xiu  |e author 
700 1 0 |a Yudong Wu  |e author 
700 1 0 |a Hongfei Jiang  |e author 
245 0 0 |a 3-aryl-4-(3,4,5-trimethoxyphenyl)pyridines inhibit tubulin polymerisation and act as anticancer agents 
260 |b Taylor & Francis Group,   |c 2024-12-01T00:00:00Z. 
500 |a 10.1080/14756366.2023.2286939 
500 |a 1475-6374 
500 |a 1475-6366 
520 |a AbstractA 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. 
546 |a EN 
690 |a Combretastatin A-4 
690 |a antiproliferative activity 
690 |a pyridine 
690 |a tubulin 
690 |a molecular docking 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 39, Iss 1 (2024) 
787 0 |n https://www.tandfonline.com/doi/10.1080/14756366.2023.2286939 
787 0 |n https://doaj.org/toc/1475-6366 
787 0 |n https://doaj.org/toc/1475-6374 
856 4 1 |u https://doaj.org/article/20346a9d73e8457f95d03cd1b57f851a  |z Connect to this object online.