PEGylation of water soluble anticancer drug, Ara-C: Syntheses and in vitro in vivo Anti-Tumor Efficacy

摘要

We designed a systematic study of N~4 PEG-prodrugs of ara-C and synthesized a series of di-, tetra-, and octa-substituted derivatives. The greater loading of the PEG backbone appears to have achieved a minimum threshold concentration for the therapeutic delivery of ara-C and showed better efficacy in both ascites and solid tumor models.