Design, synthesis and bioevaluation of novel trifluoromethylquinoline derivatives as tubulin polymerization inhibitors
Aim: A series of novel trifluoromethylquinoline derivatives were designed, synthesized and evaluated for antitumor activities. Methodology: All compounds were evaluated for antiproliferative activity against four human cancer cell lines. Results: Among them, 5a, 5m, 5o and 6b exhibited remarkable antiproliferative activities against all the tested cell lines at nanomolar concentrations. Mechanism of action studies demonstrated that 6b targeted the colchicine binding site, potentially inhibiting tubulin polymerization, and further studies indicated that 6b could arrest LNCaP cells in the G2/M phase and induce cell apoptosis. Molecular docking confirmed that 6b could bind to the colchicine binding site. Conclusion: Results suggested that 6b could serve as a promising lead compound for the development of novel tubulin polymerization inhibitors and cancer therapy.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:15 |
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| Enthalten in: |
Future medicinal chemistry - 15(2023), 21 vom: 08. Nov., Seite 1967-1986 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Zhang, Sisi [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 15.11.2023 Date Revised 29.11.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0151 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM364292776 |
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| 245 | 1 | 0 | |a Design, synthesis and bioevaluation of novel trifluoromethylquinoline derivatives as tubulin polymerization inhibitors |
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| 500 | |a Date Completed 15.11.2023 | ||
| 500 | |a Date Revised 29.11.2023 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: A series of novel trifluoromethylquinoline derivatives were designed, synthesized and evaluated for antitumor activities. Methodology: All compounds were evaluated for antiproliferative activity against four human cancer cell lines. Results: Among them, 5a, 5m, 5o and 6b exhibited remarkable antiproliferative activities against all the tested cell lines at nanomolar concentrations. Mechanism of action studies demonstrated that 6b targeted the colchicine binding site, potentially inhibiting tubulin polymerization, and further studies indicated that 6b could arrest LNCaP cells in the G2/M phase and induce cell apoptosis. Molecular docking confirmed that 6b could bind to the colchicine binding site. Conclusion: Results suggested that 6b could serve as a promising lead compound for the development of novel tubulin polymerization inhibitors and cancer therapy | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a antiproliferative activity | |
| 650 | 4 | |a antitumor | |
| 650 | 4 | |a molecular docking | |
| 650 | 4 | |a trifluoromethylquinoline derivatives | |
| 650 | 4 | |a tubulin polymerization inhibitors | |
| 650 | 7 | |a Tubulin Modulators |2 NLM | |
| 650 | 7 | |a Colchicine |2 NLM | |
| 650 | 7 | |a SML2Y3J35T |2 NLM | |
| 650 | 7 | |a Tubulin |2 NLM | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 700 | 1 | |a Mo, Min |e verfasserin |4 aut | |
| 700 | 1 | |a Lv, Mengfan |e verfasserin |4 aut | |
| 700 | 1 | |a Xia, Wen |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Kun |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Gang |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Jia |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Guangcan |e verfasserin |4 aut | |
| 700 | 1 | |a Zeng, Xiaoping |e verfasserin |4 aut | |
| 700 | 1 | |a Cheng, Sha |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Bixue |e verfasserin |4 aut | |
| 700 | 1 | |a Luo, Heng |e verfasserin |4 aut | |
| 700 | 1 | |a Meng, Xueling |e verfasserin |4 aut | |
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