土槿乙酸衍生物的合成及其抗肿瘤活性

The synthesis of Pseudolaric acid B derivatives and their antitumor activity

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 relationship between the Pseudolaric acid B structure and its antitumor activity. Methods： 8 derivatives of Pseudolaric acid B have been synthesized in this paper. Their structures were conformed by 1H - NMR,MS. The antitumor activity of the derivatives were determined by MTT methods. Results： All the 8 derivatives were not reported by previous literature. Results showed the antitumor activity of the derivatives approach to Pseudolaric acid B , the antitumor activity of the derivatives Ⅱf, g are better than Pseudolaric acid B. Conclusion： some esters and amids de of Pseudolaric acid B are necessary group in antitumor activity.