MDR逆转活性紫杉烷类化合物的合成

Synthesis of taxoids against multidrug resistant tumor cells

目的:合成天然产物taxinine NN-3和taxinine NN-14,研究其对肿瘤细胞的多药耐药逆转活性。方法:以紫杉宁为出发原料,通过选择性水解9,10位的乙酰氧基,制成原乙酸酯后再水解。结果:以紫杉宁为原料经过3步反应,可以同时获得taxinine NN-3,taxinine NN-4两种天然产物,其中taxinine NN-3的收率为25%,taxinine NN-4的收率为68%。结论:高收率地合成了taxinine NN-3和taxinine NN-14。

Objective:To synthesize taxinine NN-3 and taxinine NN-14 with biological activity against multidrug resistant (MDR) tumor cells. Methods: Starting from taxinine, taxinine NN-3 and taxinine NN-14 were synthesized via selective deacetoxylation, orthoester and hydrolysis. Results:Total yield of taxinine NN-14 was 68% and taxinine NN-4 was 25% from taxinine. Conclusion: A simple and yielding synthesis of taxinine NN-3 and taxinine NN-14 was achieved.