【摘要】 ＳｉｎｅｎｘａｎＡ（２）是一从红豆杉组织培养物中分离得到的具有紫杉醇母核Ａ／Ｂ／Ｃ环骨架的化合物。以该化合物为起始原料，通过４，２０－双键合成Ｄ－环，在１４β-位引入侧链等合成了１，７，９，１３－脱氧－１４β-侧链紫杉醇类似物４和５。这两个化合物在体外活性实验中，对ＫＢ，Ａ２７８０和ＨＣＴ－８细胞株的细胞毒性比紫杉醇显著降低；１０μｍｏｌ·Ｌ(－１)浓度下对微管蛋白聚合没有作用。更多还原

【Abstract】 Sinenxan A (2), isolated from tissue culture, possesses an A/B/C ring skeletonwithout 1,7,9,13-oxygen functionality of paclitaxel (1). Two 1,7,9,13-deoxy, C-14β side chain analogues 4 and 5 of 1 were synthesized from 2 by incorporating the 4,20-double bond into the D-ring and introducing the side chain at 14β position. Compounds 4 and 5 showed significantly decreasedactivity in the cytotoxicity assay in vitro against KB, A2780, and HCT-8. In tubulin assembly assaythey did not show any activity at 10μmol.L-1.更多还原