A novel series of chalcone derivatives containing diaryl ether moiety (5a-5p) were designed, synthesized and evaluated their anti-tubulin polymerization activities and anticancer activities. Among them, compound 5b with 4-methoxy substitution on right aromatic ring was found to be most active on MCF-7, HepG2 and HCT116 cancer cell lines, with IC50 values of 3.44 ± 0.19, 4.64 ± 0.23, and 6.31 ± 0.27 μM, respectively. In vitro tubulin polymerization assay showed that 5b could effectively inhibit tubulin polymerization. Further mechanism studies revealed that 5b could induce G2/M phase arrest and cell apoptosis. Molecular docking studies revealed that 5b interact and bind at the colchicine binding site of the tubulin.

中文翻译：

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新的查尔酮衍生物的设计，合成，生物学评估和分子对接研究，这些二查尔酮衍生物含有二芳基醚部分作为潜在的抗癌剂和微管蛋白聚合抑制剂。

设计，合成和评价了一系列含有二芳基醚部分（5a-5p）的查尔酮衍生物，并评估了它们的抗微管蛋白聚合活性和抗癌活性。其中，在右芳环上被4-甲氧基取代的化合物5b被发现对MCF-7，HepG2和HCT116癌细胞系最具活性，IC50值为3.44±0.19、4.64±0.23和6.31±0.27μM，分别。体外微管蛋白聚合试验表明5b可以有效抑制微管蛋白聚合。进一步的机制研究表明5b可以诱导G2 / M期阻滞和细胞凋亡。分子对接研究表明5b在微管蛋白的秋水仙碱结合位点相互作用并结合。