摘要
本篇文章以5-苄氧基环磷酰胺为先导化合物,通过连接臂4-羟基苄醇将肝靶向基团半乳糖基与环磷酰胺缀合,设计合成了一类5-半乳糖苷苄氧基环磷酰胺类前药1a和1b。期待从这些化合物中能筛选出具有肝靶向性和较好抗癌活性的环磷酰胺衍生物。
Novel prodrugs of cyclophosphamide 1a and 1b, which comprised the galactosyl moiety, the key fraction of cyclophosphamide derivates, and the linker 4-hydroxy benzaldehyde, were synthesized. These compounds were anticipated to exhibit amplified anti-tumor activity and targeting ability.
基金
National Natural Science Foundation of China (Grant No.20732001,90713004)
