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为了寻找高效低毒、抗瘤谱广、综合性能好又不依赖自然资源的新一代紫杉醇类抗癌药 ,以组织培养得到的紫杉烷sinenxanA为最初起始原料 ,以紫杉烷中间体 (3)和 (16 )为合成原料合成了 10位为羰基、羟基、甲氧基乙酸酯、苄氧基乙酸酯、羟乙酸酯等共 6个新的 14β 侧链紫杉醇衍生物 .并对目标化合物进行了抗肿瘤体外试验和微管蛋白聚合试验 .结果表明所有化合物对KB细胞的IC50 >10 μg ,在浓度为 10～ 5 μmol/L时对微管蛋白无聚合作用 .说明分子的 10位结构修饰对活性无明显影响 .
In order to find a new generation of paclitaxel anticancer drugs with high efficiency, low toxicity, wide spectrum of anti-tumor, good comprehensive performance and no dependence on natural resources, taxane sinenxanA obtained from tissue culture was used as initial starting material, 3) and (16) were synthesized for the synthesis of the first 10 for the carbonyl, hydroxy, methoxy acetate, benzyloxyacetate, glycolate and a total of six new 14β side chain paclitaxel derivatives and The antitumor in vitro test and the tubulin polymerization test were carried out on the target compounds.The results showed that all the compounds had an IC50 of> 10 μg against KB cells and did not polymerize tubulin at a concentration of 10 to 5 μmol / L, indicating that the molecular The 10-position structure modification has no significant effect on the activity.