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目的:研究土槿乙酸抗肿瘤作用的构效关系。方法:以土槿乙酸为原料,合成8个土槿乙酸衍生物,其结构经1H-NMR,MS证实。经MTT法筛选了衍生物的抗肿瘤活性。结果:8个化合物均为新化合物,除Ⅱc所有化合物均具有抗肿瘤活性,其中Ⅱf,Ⅱg的抗肿瘤活性显著高于土槿乙酸。结论:某些土槿乙酸酯和酰胺可提高抗肿瘤活性。
Objective: To study the structure-activity relationship of the anti-tumor effect of acetic acid in soil. Methods: Eight soil acetic acid derivatives were synthesized from soil acetic acid as raw materials. Their structures were confirmed by 1H-NMR and MS. The antitumor activity of the derivatives was screened by MTT assay. RESULTS: All 8 compounds were novel compounds. All compounds except IIc had anti-tumor activity. The anti-tumor activity of IIf and IIg was significantly higher than that of guanidine acetic acid. Conclusion: Certain terpenoid acetates and amides can increase antitumor activity.