| 田婉蓉,陈瑶,李美美,邓赟.化学通报,2022,85(5):606-612. |
| 1,3-取代吲哚-2-酮衍生物的合成与肿瘤细胞毒活性研究 |
| Synthesis and Tumor Cytotoxic Activity of 1,3-Substituted Indol-2-one Derivatives |
| 投稿时间：2021-09-28 修订日期：2021-10-22 |
| DOI： |
| 中文关键词: 1,3-取代吲哚-2-酮 亲核加成反应 肿瘤细胞毒活性 |
| 英文关键词:1,3-substituted indol-2-one nucleophilic addition reaction tumor cytotoxic activity |
| 基金项目:国家自然科学基金项目（基金项目号）,中国博士后科学基金 |
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| 中文摘要: |
| 以苯胺为原料，通过肟化、环合生成二氢吲哚-2,3-二酮，再对其进行N-烷基化、亲核加成和磺酰化反应得到目标化合物5a~5g和7a~7e。通过1H NMR、13C NMR确认其结构。此外，采用噻唑蓝 (MTT)法测试了目标化合物对乳腺癌细胞MDA-MB-231、鼠黑色素瘤细胞B16、鼠结肠癌细胞CT26三种肿瘤细胞的体外抑制活性。结果表明，目标化合物7d、7e有明显的肿瘤细胞毒活性，其中化合物7d对乳腺癌细胞MDA-MB-231的细胞毒活性比阳性药五氟尿嘧啶更强，其IC50为4.63±0.14μmol/L。实验为进一步研究具有肿瘤细胞毒活性的吲哚酮类衍生物提供参考。 |
| 英文摘要: |
| Indoline-2,3-dione was synthesized via Oximation and cyclization reaction using aniline as raw material, which was reacted with N-alkylation, nucleophilic addition and sulfonylation reactions to produce compounds 5a~5g and 7a~7e. The structure was confirmed by 1H NMR and 13C NMR. In addition, the thiazolyl blue (MTT) method was used to test the in vitro inhibitory activity of the target compounds against breast cancer cells MDA-MB-231, murine melanoma cells B16, and murine colon cancer cells CT26. The results show that the target compounds 7d and 7e have obvious tumor cytotoxic activity, and the cytotoxic activity of compound 7d against breast cancer cell MDA-MB-231 is stronger than the positive drug pentafluorouracil, with an IC50 of 4.63±0.14 μmol/L. The experiment provide references for further research on indolinone derivatives with tumor cytotoxic activity. |
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