Synthesis and antitumor evaluation of 2,3-diarylbenzofuran derivatives on HeLa cells.
Synthesis and antitumor evaluation of 2,3-diarylbenzofuran derivatives on HeLa cells.
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DOI：
10.1016/j.bmcl.2017.03.010
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发表时间：
2017-04
影响因子：
2.7
通讯作者：
Guo-Xue He;Jing-Mei Yuan;Haiping Zhu;Kai Wei;Ling-Yun Wang;Shi-Lin Kong;Dong-Liang Mo;Cheng-Xue Pan
中科院分区：
文献类型：
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作者：
Guo-Xue He;Jing-Mei Yuan;Haiping Zhu;Kai Wei;Ling-Yun Wang;Shi-Lin Kong;Dong-Liang Mo;Cheng-Xue Pan
2,2-Dihydroxyarylethanones, readily prepared from the commercially available aromatic ethyl ketones, were reacted with resorcinol, 3-methoxyphenol or 2-methoxyphenol in multi steps one-pot manner promoted by trifluoroacetic acid to furnish the 2,3-diarylbenzofuran derivatives in 22–95% yield. Sixteen targeted compounds were synthesized and characterized by1H NMR,13C NMR and HRMS. MTT assay indicated that most compounds possessed effectively inhibitory activities against the proliferation of HeLa cell. Among them,4fhad the highest inhibitory activities, with the IC50being 13.40 ± 2.04 µmol/L. Cell cycle analysis, Annexin V-FITC/propidium iodide dual staining assay and western blotting analysis revealed that4finhibited the proliferation of Hela cell through apoptosis induction in a dose-dependent manner via obviously up-regulated the levels of Bak and Bim, while striking down-regulated the level of Bcl-2 and Bcl-xL protein.
