| 王平,王晓晶,潘小霞,杨淬,黄超.化学通报,2018,81(4):355-360. |
| 斑蝥素衍生物的合成、抗肝癌活性及构效关系研究 |
| Synthesis and Structure-Activity Relationship Study on Anti-Hepatoma Activity of Cantharidin Derivatives |
| 投稿时间：2017-12-14 修订日期：2018-01-02 |
| DOI： |
| 中文关键词: 斑蝥素衍生物 合成 抗肝癌 构效关系 |
| 英文关键词:Cantharidin derivatives, Synthesis, Anti-Hepatoma, Structure-activity relationship |
| 基金项目:国家自然科学基金项目（21202142，21662046） |
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| 中文摘要: |
| 基于斑蝥素衍生物结构的多样性及其良好的抗肝癌活性，本研究以呋喃、顺丁烯二酸酐为原料，合成35个斑蝥素衍生物。以顺铂为阳性对照药，经MTT法对人肝癌HepG2细胞进行初步体外抗肿瘤活性研究。测试表明：6d、6f、6g、6h、6i的抗肝癌活性与顺铂阳性对照药相当。斑蝥素酰亚胺类化合物具有较好的抗肝癌活性，且当取代基为吸电子基或含氮杂环时，化合物显现出较强的抗肝癌活性，具有潜在的抗肝癌活性及应用价值。 |
| 英文摘要: |
| Based on the diversity of the structures of cantharidin derivatives and its excellent anti-hepatoma activity, thirty-five cantharidin derivatives have been synthesized starting from furan and maleic anhydride. The anti-hepatoma activities in vitro of the synthesized compounds were evaluated against HepG2 cell by the MTT assay. The biological results demonstrated that compound 6d, 6f, 6g, 6h and 6i were commensurate with cisplatin in anti-hepatoma activity. The cantharidin imides showed good anti-hepatoma activity on the whole, and when the substituent for the electron withdrawing group and nitrogen containing heterocycles showed higher anti-hepatoma activity, so they may have potential application in anti-hepatoma drug discovery. |
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