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Currently, no inhibitors of this specific class are approved for clinical use. In this study, a series of novel 2\u2010trifluoromethyl\u20104\u2010aminoquinoline derivatives were designed, synthesized, and evaluated for their antiproliferative activity. Among them, compound\n                    <jats:bold>8a<\/jats:bold>\n                    was the most potent against LNCaP cells with an IC\n                    <jats:sub>50<\/jats:sub>\n                    value of 1\u00a0nM. Mechanistic studies demonstrated that\n                    <jats:bold>8a<\/jats:bold>\n                    disrupted tubulin polymerization by binding to the colchicine site of tubulin. Meanwhile,\n                    <jats:bold>8a<\/jats:bold>\n                    could induce cell apoptosis. Molecular docking indicated that\n                    <jats:bold>8a<\/jats:bold>\n                    could bind well to the amino acid residues in microtubule protein cavities. Overall, these findings suggested that compound\n                    <jats:bold>8a<\/jats:bold>\n                    could be a promising antitumor agent targeting the tubulin colchicine binding site.\n                  <\/jats:p>","DOI":"10.1002\/cbdv.71420","type":"journal-article","created":{"date-parts":[[2026,6,15]],"date-time":"2026-06-15T09:21:02Z","timestamp":1781515262000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Anticancer Activity of Novel Trifluoromethylquinoline Derivatives Designed to Target the Tubulin Colchicine Binding Site"],"prefix":"10.1002","volume":"23","author":[{"given":"Xiangkai","family":"Kong","sequence":"first","affiliation":[{"name":"State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine &amp; School of Pharmaceutical Sciences Guizhou Medical University  Guiyang China"},{"name":"Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&amp;D  Guiyang P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yu","family":"Su","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine &amp; School of Pharmaceutical Sciences Guizhou Medical University  Guiyang China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Siyu","family":"He","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine &amp; School of Pharmaceutical Sciences Guizhou Medical University  Guiyang China"},{"name":"Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&amp;D  Guiyang P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lei","family":"Tang","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine &amp; School of Pharmaceutical Sciences Guizhou Medical University  Guiyang China"},{"name":"Guizhou Provincial Key Laboratory of Innovation and Manufacturing for Pharmaceuticals Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&amp;D  Guiyang P.R. China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xueling","family":"Meng","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine &amp; School of Pharmaceutical Sciences Guizhou Medical University  Guiyang China"},{"name":"State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, School of Pharmaceutical Sciences, Natural Products Research Center of Guizhou Province Guizhou Medical University  Guiyang China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2026,6,15]]},"reference":[{"key":"e_1_2_9_2_1","doi-asserted-by":"publisher","DOI":"10.3322\/caac.21834"},{"key":"e_1_2_9_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2022.105770"},{"key":"e_1_2_9_4_1","doi-asserted-by":"publisher","DOI":"10.1039\/D0RA05594H"},{"key":"e_1_2_9_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2021.105105"},{"key":"e_1_2_9_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tcb.2018.05.001"},{"key":"e_1_2_9_7_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.1168823"},{"key":"e_1_2_9_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2015.06.049"},{"key":"e_1_2_9_9_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.0c00222"},{"key":"e_1_2_9_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.tibs.2009.09.002"},{"key":"e_1_2_9_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2014.02.035"},{"key":"e_1_2_9_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2014.09.051"},{"key":"e_1_2_9_13_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.1c00100"},{"key":"e_1_2_9_14_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrd3253"},{"key":"e_1_2_9_15_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.9b00551"},{"key":"e_1_2_9_16_1","doi-asserted-by":"publisher","DOI":"10.1039\/c0ib00135j"},{"key":"e_1_2_9_17_1","doi-asserted-by":"publisher","DOI":"10.1002\/ddr.20267"},{"key":"e_1_2_9_18_1","doi-asserted-by":"publisher","DOI":"10.1039\/D3RA02904B"},{"key":"e_1_2_9_19_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.6b00463"},{"key":"e_1_2_9_20_1","doi-asserted-by":"publisher","DOI":"10.1124\/jpet.115.226225"},{"key":"e_1_2_9_21_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.amjmed.2014.12.010"},{"key":"e_1_2_9_22_1","doi-asserted-by":"publisher","DOI":"10.5694\/mja14.00846"},{"key":"e_1_2_9_23_1","first-page":"3408","article-title":"A Phase I Pharmacokinetic and Translational Study of the Novel Vascular Targeting Agent Combretastatin a\u20104 Phosphate on a Single\u2010Dose Intravenous Schedule in Patients With Advanced Cancer","volume":"62","author":"Dowlati A.","year":"2002","journal-title":"Cancer Research"},{"key":"e_1_2_9_24_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm8003653"},{"key":"e_1_2_9_25_1","doi-asserted-by":"publisher","DOI":"10.1097\/CAD.0b013e32832c0acf"},{"key":"e_1_2_9_26_1","first-page":"3208","article-title":"Mechanism of Action of E7010, an Orally Active Sulfonamide Antitumor Agent: Inhibition of Mitosis by Binding to the Colchicine Site of Tubulin","volume":"57","author":"Yoshimatsu K.","year":"1997","journal-title":"Cancer Research"},{"key":"e_1_2_9_27_1","doi-asserted-by":"publisher","DOI":"10.1517\/13543776.2014.859247"},{"key":"e_1_2_9_28_1","doi-asserted-by":"publisher","DOI":"10.2174\/0929867322666150114163732"},{"key":"e_1_2_9_29_1","doi-asserted-by":"publisher","DOI":"10.4155\/fmc-2023-0151"},{"key":"e_1_2_9_30_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bmc.2025.118472"},{"key":"e_1_2_9_31_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.1c01451"}],"container-title":["Chemistry &amp; 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