蛇床子素二苯乙烯类衍生物的合成及抑制微管蛋白聚合作用

Synthesis and tubulin polymerization inhibitory activity of osthol stilbene derivatives

摘要: 以蛇床子素为先导化合物，合成了6个目标化合物（ Ⅵ_1-5、Ⅵ₇ ），其结构经MS及¹H NMR确证；通过抗人脐静脉内皮细胞（HUVEC）体外增殖的实验，测定了目标物抑制微管蛋白聚合的活性。结果表明，所合成的化合物多数具有一定的抑制微管蛋白聚合的作用，其中化合物 Ⅵ₇ 的活性最强，值得进一步深入研究。

Abstract: A series of novel osthole stilbene derivatives were synthesized,and their structures were determined by MS and ¹H NMR.The tubulin polymerization inhibitory activity of the synthesized compounds was evaluated using anti-human umbilical vein endothelial cells in vitro.Preliminary results showed that compound Ⅵ₇ was the most potent inhibitor,but was less potent than combretastatin A-4.Compound Ⅵ_7 is a promising compound worthy of further studies.