东莨菪素衍生物的设计、合成及抗增殖活性

Design, synthesis and antiproliferative activity of scopoletin derivatives

摘要: 对东莨菪素的3位进行结构修饰，通过引入不同取代的苯甲酰胺基团，设计并合成了9个未见文献报道的新化合物( 10a~10i )，其结构经ESI-MS、IR和¹H NMR确认。采用MTT法评价了化合物对MCF-7、A549及HCT-116肿瘤细胞的抗增殖作用。结果表明，部分化合物对肿瘤细胞具有较好抗增殖作用，其中化合物 10g 抗增殖活性最强，强于阳性对照药东莨菪素和舒尼替尼。

Abstract: To explore novel scopoletin derivatives with more potent antiproliferative activity, a series of compounds were designed and synthesized( 10a - 10i )by linking benzamide to scopoletin′s framework. Their structures were determined by ESI-MS, IR and ¹H NMR. The antiproliferative activity of the synthetic derivatives against human cancer cells MCF-7, A549 and HCT-116 was evaluated by MTT assay. Preliminary experimental results showed that compound 10g was the most potent one, whose antiproliferative activity was stronger than that of the positive control scopoletin and sunitinib.