| 王妙,黄琳,苏燕,许英红,黄铃月,周小群b,李芳耀a.化学通报,2019,82(7):630-635. |
| 丹皮酚噻唑类化合物的合成及其细胞毒性评价 |
| Synthesis and Cytotoxicity Evaluation of Novel Paeonol-Thiazoles Derivatives |
| 投稿时间：2019-01-31 修订日期：2019-02-15 |
| DOI： |
| 中文关键词: 丹皮酚 噻唑 合成 抗肿瘤活性 |
| 英文关键词:Paeonol, Thiazole, Synthesis, Antitumor activity |
| 基金项目:广西自然科学基金项目(2016GXNSFAA380323, 2018GXNSFAA281200)，广西自然科学基金重大项目(2016GXNSFEA380001)，国家级大学生创新创业训练计划项目(201710601017)，桂林市科学研究与技术开发计划重点项目(20170108-10)，广西高校中青年科研基础能力提升项目(2019KY051)，广西肿瘤免疫与微环境调控重点实验室开放课题(2018KF010) |
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| 中文摘要: |
| 本文以丹皮酚为原料合成了15个新型丹皮酚噻唑衍生物，利用IR、1H-NMR、13C-NMR和MS对所得化合物的结构进行表征，采用MTT法考察了目标化合物对MGC-803（胃癌细胞）、LOVO（结肠癌细胞）、T-24（膀胱癌细胞）3种细胞的体外抗肿瘤活性，结果表明部分目标产物具有良好的细胞毒活性，其中化合物4d、4f、4h、4m、4n对MGC-803的细胞毒性优于阳性对照药顺铂，尤其是化合物4h对MGC-803、LOVO和T-24三种肿瘤细胞的IC50值分别为11.39±4.46，2.06±1.27和6.03±0.86，值得进一步研究。 |
| 英文摘要: |
| A series of novel paeonol thiazole derivatives were synthesized using paeonol as starting material and their structures were confirmed by IR, 1H-NMR, 13C-NMR and MS. All of them were evaluated for their antitumor activities against three human cancer cell lines (MGC-803, LOVO and T-24) in vitro by standard MTT assay. The results presented that some of the target compounds exhibit significant cytotoxic activity, such as compounds 4d, 4f, 4h, 4m, 4n exhibited better antitumor activity than the positive reference cisplatin against MGC-803. In particular, compound 4h showed the most potent antitumor activities with IC50 values of 11.39±4.46,2.06±1.27and 6.03±0.86 against MGC-803, LOVO and T-24 tumor cell lines, respectively. It suggested that 4h might be the candidate for further investigation. |
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