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，进行了构效关系研究，发现BKA的三个羧酸基团在星形孢菌素诱导的HeLa细胞凋亡抑制活性中起重要作用。接下来，我们设计合成了结构简单的衍生物和构象受限的衍生物，发现这些衍生物具有较强的细胞凋亡抑制活性。因此，我们成功地实现了更容易获得的有效的新型凋亡抑制剂的设计和合成，这将是有用的高灵敏度的荧光探针。基于高立体选择性的共轭烯丙基化反应，实现了黄嘌呤的高效不对称合成。

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.