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目的:设计、合成具有双迈克尔受体结构单元的齐墩果酸衍生物并研究其体外抗肿瘤活性。方法:以齐墩果酸为原料,经过酰化、酯化、水解、氧化以及醇醛缩合反应得到目标化合物;采用MTT法在白血病HL-60,肝癌SMMC-7721,肺癌A-549,乳腺癌MCF-7,结肠癌SW480细胞株上进行了体外抗肿瘤活性的测试。结果:合成了一个具有双迈克尔受体结构单元的新齐墩果酸衍生物,并经过1H-NMR,13C-NMR,ESI-MS确证了化学结构。结论:初步的体外抗肿瘤活性显示,该化合物具有较好的抗肿瘤活性,在结肠癌SW480细胞株上较为明显。
OBJECTIVE: To design and synthesize oleanolic acid derivatives with double Michael acceptor structural units and to study their anti-tumor activity in vitro. METHODS: Oleanolic acid was used as the starting material to get the target compound through acylation, esterification, hydrolysis, oxidation and aldol reaction. The target compounds were obtained by MTT assay in HL-60, SMMC-7721, A-549, MCF-7, colon cancer SW480 cell line in vitro anti-tumor activity of the test. Results: A novel oleanolic acid derivative with a double Michael acceptor unit was synthesized and confirmed by 1H-NMR, 13C-NMR and ESI-MS. Conclusion: The preliminary in vitro anti-tumor activity shows that the compound has good anti-tumor activity, which is more obvious in colon cancer SW480 cell line.