紫杉醇类似物的合成及抗肿瘤活性  

SYNTHESIS AND CYTOTOXICITY OF THE NEW TAXOIDS

作　　者：要芬梅 郭积玉[1] 梁晓天[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所

出　　处：《药学学报》1998年第9期659-665,共7页Acta Pharmaceutica Sinica

摘　　要：ＳｉｎｅｎｘａｎＡ（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。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 C14 or C10 positions with taxol/taxotere side chain. Preliminary pharmacological tests showed that some of the compounds have certain cytotoxicity on KB, HCT8 and A2780. Meanwhile, the relationship between their structures and activity was discussed.

关 键 词：抗肿瘤活性 紫杉醇 类似物 合成 

分 类 号：TQ464.9[化学工程—制药化工] R979.1[医药卫生—药品]