Structure-activity relationship study of hybrid acetogenins toward the practical use

我们计划探索最近发现的新型抗癌先导化合物的杂化乙酰原的作用模式。以2,5-二甲酰基四氢呋喃为原料，用荧光基团标记的炔和噻吩环标记的炔进行了两次不对称炔基化，实现了荧光标记杂化乙酰原的会聚合成。标记的杂交乙酰源蛋白和MitoTracker Red的合并荧光表明，杂交乙酰源蛋白定位于线粒体。并合成了末端氨基衍生物，用于亲和柱层析。

We planed the exploring mode of action of hybrid acetogenins that we recently found novel lead compounds for anticancer agents. The convergent synthesis of fluorescence-labeled hybrid acetogenin was accomplished by two asymmetric alkynylations of 2,5-diformyl tetrahydrofuran with an alkyne tagged with fluorescent groups and another alkyne with thiophen ring. The merged fluorescence of labeled hybrid acetogenin and MitoTracker Red suggests that hybrid acetogenins localize in the mitochondria. The derivative with terminal amino group was also synthesized for affinity column chromatography.