| 吉礼涛,邱雪梅,谭画元,王钦,李焱,戈强胜,王贞超,李成朋.化学通报,2023,86(5):612-616. |
| 具有砜结构的吲哚衍生物的合成及生物活性研究 |
| Synthesis and biological activity of indole derivatives with sulfone structureJi Litao1,? Qiu Xuemei1,? Tan Huayuan1, Wang Qin1,? Li Yan1,? Ge Qiangsheng1, Wang Zhenchao1,2,3*,? Li Chengpeng1,2,3* |
| 投稿时间：2022-08-11 修订日期：2022-12-02 |
| DOI： |
| 中文关键词: 吲哚衍生物 肿瘤细胞毒活性 植物病原菌 |
| 英文关键词:indole derivatives, tumor cytotoxic activity, plant pathogens |
| 基金项目:国家自然科学基金项目(21867004,22007022)和贵州省教育厅重点项目(QjhKYZi[2021]No.041)资助 |
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| 中文摘要: |
| 以吲哚-3-羧酸甲酯为原料，通过肼解、环合生成5-(3-1H-吲哚基)-1,3,4-噁二唑-2-硫醇，再对其进行亲核取代和氧化反应得到目标化合物，并通过1H-NMR、13C-NMR、HRMS确认其结构。我们采用噻唑蓝（MTT）法测试了目标化合物对几种癌细胞的体外抑制活性，同时采用比浊法对几种植物病原菌进行了体外抑菌活性测试。结果表明，化合物对于A549（人肺腺癌细胞）、PC-3（人前列腺癌细胞）、K562（人慢性髓原白血病细胞）和HepG2（人肝癌细胞）四种癌细胞有一定的抑制活性。对水稻白叶枯病菌（Xanthomonas oryzae pv.oryzae，Xoo）、柑橘溃疡病菌（Xanthomonas axonopodis pv. citri，Xac）以及猕猴桃溃疡病菌（Pseudomonas syringae pv. actinidiae，Psa）四种植物病菌同样具有一定的抑菌活性。其中，化合物4f对Xoo的体外抑制率可达到87.09 % （100 μg/mL）和54.02 % （50 μg/mL）。本文结果可为进一步研究具有砜结构的吲哚衍生物的合成及应用提供参考。 |
| 英文摘要: |
| With methyl indole-3-carboxylate as raw material, 5 - (3-1H-indolyl) - 1,3,4-oxadiazole 2-mercaptan was synthesized by hydrazinolysis and cyclization, and then nucleophilic substitution and oxidation reaction were carried out to obtain the target compound, and their chemical structures were confirmed by 1H-NMR, 13C-NMR, and high-resolution mass spectrometry. The anti-proliferation activity of them against several cancer cells in vitro were tested by thiazole blue (MTT) method, and their antibacterial activity against several plant pathogens in vitro were tested by turbidimetry.The results showed that the compounds had certain inhibitory activity on A549 (human lung adenocarcinoma cell), PC-3 (human prostate cancer cell), K562 (human chronic myelogenous leukemia cell) and HepG2 (human liver cancer cell). It also has antibacterial activity against Xoo (Xanthomonas oryzae pv.oryzae), Xac (Xanthomonas axonopodis pv. citri) and Psa (Pseudomonas syringae pv. actinidiae).Among them, the inhibitory rate of compound 4f on Xoo in vitro can reach 87.09% (100 μg/mL) and 54.02% (50 μg/mL). These findings can provide a reference for the further study of the synthesis and application of indole derivatives with sulfone structure. |
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