化学
部分
立体化学
微管蛋白
细胞毒性
对接(动物)
二苯甲酮
质子核磁共振
组合化学
体外
微管
生物化学
有机化学
细胞生物学
生物
护理部
医学
作者
Guangcheng Wang,Wenjing Liu,Juan Tang,Xue Ma,Zipeng Gong,Yong Huang,Yongjun Li,Zhiyuan Peng
标识
DOI:10.1016/j.bioorg.2020.104265
摘要
A series of benzophenone derivatives bearing naphthalene moiety were designed, synthesized, characterized by 1H NMR, 13C NMR, and HRMS and evaluated for their antiproliferative activity against human breast cancer cell line (MCF-7). Most of the tested derivatives showed good to moderate cytotoxicity against MCF-7 cell line. Among them, compound 4u (IC50 = 1.47 ± 0.14 μM) was found to be the most active compound, which is more active than the standard drug cisplatin (IC50 = 15.24 ± 1.27 μM). In vitro tubulin polymerization inhibition assay, EBI competition assay, cell cycle analysis, and cell apoptosis assay identified that compound 4u was a new tubulin polymerization inhibitor by targeting the colchicine binding site. Besides, molecular docking study showed that compound 4u has high binding affinities with the colchicine binding site of tubulin through hydrogen bond, cation-π, and hydrophobic interaction.
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