土槿乙酸衍生物的合成及其抗肿瘤活性研究

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16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。结果其中14个化合物为新化合物,衍生物IIa,b,c,d,e,f,g的抗肿瘤活性与土槿乙酸类似,而其部分水解产物的抗肿瘤活性均明显低于土槿乙酸。结论4位乙酰氧基,7位甲酯为土槿乙酸抗肿瘤活性所必需基团。

To study-the relationship between pseudolaric acid B structm＇e am its antitumor activity. Methods Sixteen derivatives of pseudolaric acid B were synthesized. Their structures were identified by＂ 1H - NMR and MS. The antitumor activities of the derivatives were determined by＂ MTr assay. Resultant 14 of the 16 derivatives have not been reported in previous literature. Results The antitumor activities of the derivatives Ⅱ a, b, c, d, e, f, g am similar to that of pseudolaric acid B, but those of the derivatives Ⅲ a, b, c, d and ⅥIV a, b, c, d are lower than that of pseudolaric acid B. Conclusions 4 - acetoxy and 7 -methyl ester of pseudolaric acid B are the essential group of pseudolaric acid B in antitumor activity.