| 李红侠,钱玉梅,王海潮,单玲玲.化学通报,2019,82(10):909-916. |
| 2-巯基苯并咪唑衍生物的设计、合成及抗肿瘤活性研究 |
| Design, synthesis and biological evaluation of 2-thiol benzimidazole derivatives as potential anticancer agents |
| 投稿时间：2019-04-22 修订日期：2019-07-10 |
| DOI： |
| 中文关键词: 苯并咪唑衍生物 抗肿瘤活性 表皮生长因子抑制剂 |
| 英文关键词:Benzimidazole derivatives Anti-tumor activity EGFR inhibitors |
| 基金项目:安徽省自然科学重点项目（KJ2017A441）、宿州学院自然科学重点项目（2017yzd11，2016yzd04）、安徽省科技厅自然科学基金项目（1808085MG256，1908085MC100)资助 |
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| 中文摘要: |
| 为了从苯并咪唑类衍生物中寻找新的活性化合物, 以溴乙酸作为起始原料，设计合成了17个2-巯基苯并咪唑衍生物4a-4q. 采用噻唑蓝（MTT）法测试了目标化合物对人宫颈癌细胞(HeLa)、人乳腺癌细胞(MCF-7)、 人肝癌细胞(HepG2)、人非小细胞肺癌细胞（A549）的细胞增殖抑制活性，流式细胞仪检测细胞凋亡。 结果显示大部分化合物具有较好的抗肿瘤活性，其中((1H-苯并[d]咪唑-2-基)硫基)-1-(4-(2-甲氧基苯基)哌嗪-1-基)乙烷-1-酮（4n）对HepG2细胞的抑制活性最好，IC50值为12.62±0.78 μmol/L, 接近于对照药品吉非替尼(9.72±.038 μmol/L)。此外，利用分子对接方法，对目标化合物的构效关系进行了讨论。 |
| 英文摘要: |
| In order to find novel benzimidazole derivatives having potent bioactivities, a series of novel 2-thiol benzimidazole derivatives (4a-4q) were designed and synthesized from the starting material of bromide acetic acid. The cell antiproliferative activities against human cervical cancer cell line (Hela), human breast cancer cells (MCF-7), human hepatoma cells (HepG2) and human non-small cell lung cancer cell lines cells (A549) were estimated in vitro via thiazolyl blue tetrazolium bromide (MTT) assay method.The flow cytometry to examine cell apoptosis rate. The test results showed that most target compounds exhibited moderate antitumor activities，especially the compound
2-((1H-benzo[d]imidazol-2-yl)thio)-1-(4-benzhydrylpiperazin-1-yl)ethan-1-one(4l) possessed stronger inhibitory activity against HepG2 cell lines with the IC50 value of 12.62±0.78 μmol/L， exhibiting is close to than the control Gefitinib (11.72±.038 μmol/L). Moreover, the structure-activity relationship (SAR) of the derivatives was discussed by docking studies. |
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