PRODRUGS BASED ON GEMCITABINE STRUCTURE AS WELL AS SYNTHETIC METHOD AND APPLICATION THEREOF

摘要

Prodrugs based on gemcitabine structure shown as formula (I) as well as their synthetic method and application are disclosed, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is solved and intestinal toxicity induced by gemcitabine is decreased. As a result, the prodrugs can be delivered by oral administration and further improve their antagonistic capacity in respect of tumors, cancer, infection and diffusion, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.