Research on Anti-Tumor Active Site of Marine Source Compound, Halichondrin

我们成功地建立了一条从廉价的商业原料中分离得到的高强度抗癌聚醚大环内酯的大内酯部分和聚醚部分的一条灵活高效的合成路线。比较了合成中间体中的两个聚醚单元化合物对KB和L1210的体外细胞毒作用。研究发现，聚醚单元第一次显示出相当强的细胞毒性，尽管这两个被检查的化合物的活性没有天然的何首乌B那么高。

We succeeded in establishing a flexible and efficient synthetic pathway of macrolactone part and the polyether part of the highly strong antitumor polyether macrolide, halichondrin B, isolated from cheap and commercially available starting materials. Two compounds, a part of polyether unit, in our synthetic intermediates were compared by cytotoxity against KB and L1210 in vitro . It found that the polyether unit indicated considerably strong cytotoxity for the first time although the activities of the two examined compounds were not so high as those of the natural halichondrin B.