紫杉醇类似物的合成及抗肿瘤活性
SYNTHESIS AND CYTOTOXICITY OF THE NEW TAXOIDS
-
摘要: Sinenxan A(SIA)为生物合成法得到的新紫杉烷化合物。为寻找有抗肿瘤活性的新型taxol类似物,对SIA进行结构修饰.设计合成了10个化合物,在母核中引入四氢呋喃环,在14β-位或10β-位连接taxol/taxotere侧链,部分化合物显示一定的抗肿瘤活性。并讨论了这类化合物的构效关系。Abstract: Sinenxan A is a new biosynthetic taxane. In order to search for new taxol analogues with cytotoxicity, sinenxan A was modified and studied.Ten new taxoids containing the tetrahydrofuran ring were esterified at C14 or C10 positions with taxol/taxotere side chain. Preliminary pharmacological tests showed that some of the compounds have certain cytotoxicity on KB, HCT-8 and A2780. Meanwhile, the relationship between their structures and activity was discussed.
下载: