Development of highly sensitive fluorescent probes based on Quantum dot labeling

在我们开发的BKA全合成的基础上，我们进行了构效关系研究，发现BKA的三个羧基在星状孢子素诱导的HeLa细胞凋亡抑制活性中起着重要作用。接下来，我们设计并合成了更简单的衍生物和构象受限的衍生物，发现这些衍生物具有很强的细胞凋亡抑制活性。因此，我们成功地设计和合成了更容易获得的有效的新型细胞凋亡抑制剂，这将有助于高灵敏的荧光探针。基于&#61543；-丁烯内酯的高立体选择性共轭烯丙基化反应，实现了黄原素的高效不对称合成。

Based on our developed total synthesis of BKA, we conducted the structure-activity relationship study, which revealed three carboxylic acid groups of BKA plays an important role in staurosporin-induced apoptosis inhibitory activity of HeLa cells. Next, we designed and synthesized simpler derivatives and the conformation-restricted derivatives and then found that these derivatives showed potent apoptosis inhibitory activity. Consequently, we successfully achieved the design and synthesis in more easily available potent novel apoptosis inhibitors, which would be useful for highly sensitive fluorescent probes. The efficient asymmetric synthesis of xanthatin based on the highly stereoselective conjugate allylation of the -butenolide was also achieved.