Synthesis Of Several Cluster Galactosides And Study Of Their Bioactivities

In this dissertation, a series of cluster galactosides have been investigated, including the synthesis and the study of liver targeting. The structures of these target compounds were confirmed by ¹H NMR, ¹³3C NMR. COSY, HMQC respectively. The contents and the primary contributions of the research are summarized as follows:(1) A series of cluster galactosides with different scaffolds were synthesized. The affinity of these compounds for ASGPR was analyzed by binding study in vitro. The results showed that trivalent cluster galactosides behaved better than divalent analogues and the cluster galactosides with aryl groups on their scaffolds presented better binding affinity than those with aliphatic chain scaffolds.(2) An ultraviolet spectrophotometric method for the determination of liver targeting was developed by the reaction of galactosides with dansyl chloride. The results show that the method is simple, rapid and feasible. Furthermore, cluster effect was confirmed once again through this method.(3) Two kinds of galactosides containing 5-flurouracil were synthesized and their in vitro antitumor activities have been tested by MTT. The results indicate that these compounds show almost the same antitumor activities as 5-flurouracil. The further work still need to be done.