微管蛋白
LNCaP公司
化学
秋水仙碱
作用机理
微管
对接(动物)
微管聚合
细胞凋亡
细胞培养
细胞生长
癌细胞
生物化学
体外
药理学
癌症
生物
细胞生物学
医学
遗传学
护理部
作者
Si-Si Zhang,Min Mo,Mei Lv,Xin Wen,Kun Liu,Gang Yu,Jia Yu,Guang-can Xu,Xiaoping Zeng,Sha Cheng,Bixue Xu,Heng Luo,Xueling Meng
出处
期刊:Future Medicinal Chemistry
[Newlands Press Ltd]
日期:2023-11-01
卷期号:15 (21): 1967-1986
标识
DOI:10.4155/fmc-2023-0151
摘要
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.
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