紫杉烷类化合物 SINENXAN A 的结构修饰及其衍生物的构效关系研究

STUDIES ON STRUCTURE MODIFICATION ANDSTRUCTUREACTIVITY RELATIONSHIP OF NEW TAXOIDS DERIVED FROM SINENXAN A

为寻找新的综合性能好的紫杉烷类化合物，对ｓｉｎｅｎｘａｎＡ（ＳＩＡ）进行结构修饰。在ＳＩＡ及其修饰物的Ｃ１４位引入不同的的侧链，共合成新的紫杉醇类似物２１个，对其中的１５个化合物进行了３种癌细胞的体外抗肿瘤活性测定，这些化合物的活性与紫杉醇比较，相差甚远。本文初步讨论了ＳＩＡ衍生物的构效关系。

In order to develop new taxol analogues with possible antitumor properties, sinenxan A (SIA), a new biosynthetic taxoid, was chemically modified, mainly by esterification of C14OH with taxollike sidechain acids. Twentyone new taxoids thus formed were tested on three kinds of cell lines. Their activities are far below those of taxol. The SAR of SIA derivatives partly agree with that of taxol and can be roughly discerned.