Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents†,RSC Medicinal Chemistry

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Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-12-27 00:00:00 , DOI: 10.1039/c7md00578d
Zhe Wang _{1,

2,

3,

4,

5} , Xiangping Deng _{1,

2,

3,

4,

5} , Runde Xiong _{1,

2,

3,

4,

5} , Shujuan Xiong _{1,

2,

3,

4,

5} , Juan Liu _{1,

2,

3,

4,

5} , Xuan Cao _{1,

2,

3,

4,

5} , Xiaoyong Lei _{1,

2,

3,

4,

5} , Yanming Chen _{5,

6,

7} , Xing Zheng _{1,

2,

3,

4,

5} , Guotao Tang _{1,

2,

3,

4,

5}

Affiliation

A series of 3′,4′,5′-trimethoxy flavonoids with benzimidazole linked by different chain alkanes have been designed and synthesized. The potential activity of these compounds as anti-tumor agents was evaluated by cytotoxicity assay in MGC-803 (human gastric cancer), MCF-7 (human breast cancer), HepG-2 (human hepatoma) and MFC (mouse gastric cancer) tumor cell lines. Among them, compound 15 7-(3-(2-chloro-1H-benzo[d]imidazol-1-yl)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one displayed the most potent antiproliferative activity, with IC₅₀ values of 20.47 ± 2.07, 43.42 ± 3.56, 35.45 ± 2.03 μM and 23.47 ± 3.59 μM, respectively. The flow cytometry (FCM) results showed that compound 15 caused the cell cycle to be arrested in G1 phase and induced apoptosis of MFC cells in a dose-dependent manner. In addition, compound 15 exhibited a significant inhibitory effect on tumor growth in vivo. All the results outlined the great potential of compound 15 for further exploitation as anti-tumor agent.

中文翻译：

3'，4'，5'-三甲氧基黄酮类苯并咪唑衍生物作为潜在抗肿瘤药的设计，合成和生物学评价†

设计并合成了一系列苯并咪唑通过不同链烷烃连接的3'，4'，5'-三甲氧基黄酮类化合物。这些化合物作为抗肿瘤药的潜在活性通过MGC-803（人类胃癌），MCF-7（人类乳腺癌），HepG-2（人类肝癌）和MFC（小鼠胃癌）肿瘤中的细胞毒性试验进行了评估。细胞系。其中，化合物15 7-（3-（2-氯-1 H-苯并[ d ]咪唑-1-基）丙氧基）-2-（3,4,5-三甲氧基苯基）-4 H-铬烯-4-一种显示最有效的抗增殖活性，IC ₅₀值分别为20.47±2.07、43.42±3.56、35.45±2.03μM和23.47±3.59μM。流式细胞仪（FCM）结果表明化合物15导致细胞周期停滞在G1期，并以剂量依赖性方式诱导MFC细胞凋亡。另外，化合物15对体内肿瘤生长显示出显着的抑制作用。所有结果概述了化合物15作为抗肿瘤剂的进一步开发的巨大潜力。

更新日期：2017-12-27

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