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目的:设计合成新型去甲斑蝥素衍生物,并研究其体外抗肿瘤活性。方法:以呋喃和马来酸酐为起始原料经多步反应合成去甲斑蝥素衍生物,化合物经1HNMR、ESI-MS和元素分析确证结构;用MTT法,首先对所有化合物进行抗乳腺癌细胞株4T1体外活性筛选,然后对活性较好的化合物7a和7c进一步作抗肺癌细胞株LLC和抗肝癌细胞株SK-HEP-1的活性检测,同时对这2种化合物进行对正常血管内皮细胞ABAE的损伤试验。结果:设计合成了18种新化合物。其中化合物7a和7c对肿瘤细胞株有一定的抑制作用,而对正常细胞的损伤程度较低。结论:化合物7a和7c对乳腺癌细胞株4T1、肺癌细胞株LLC和肝癌细胞株SK-HEP-1有一定的抑制作用,尤其是化合物7c对正常内皮细胞ABAE的损伤比对照药去甲斑蝥素小得多,有进一步研究的价值。
OBJECTIVE: To design and synthesize a novel norcantharidin derivative and study its antitumor activity in vitro. Methods: Norcantharidin derivatives were synthesized from furan and maleic anhydride by multistep reaction. The compounds were confirmed by 1HNMR, ESI-MS and elemental analysis. MTT assay was performed on all compounds against breast cancer cells Strain 4T1 was screened in vitro. Then the more active compounds 7a and 7c were further tested for anti-lung cancer cell line LLC and anti-liver cancer cell line SK-HEP-1. At the same time, these two compounds were tested against normal vascular endothelial cells ABAE Damage test. Results: 18 new compounds were designed and synthesized. Among them, compounds 7a and 7c had some inhibitory effect on tumor cell lines, but lower damage to normal cells. CONCLUSION: Compounds 7a and 7c have some inhibitory effects on breast cancer cell line 4T1, lung cancer cell line LLC and hepatocellular carcinoma cell line SK-HEP-1. In particular, compound 7c harms normal endothelial cells ABAE more than norcantharidin Much smaller, with further research value.