3 years ago

Synthesis and biological activities of galactose–aspirin conjugate prodrug designed for ADEPT and PMT

Gangliang Huang

Abstract

Aspirin was used as the lead compound, and its structure was modified by galactosylation. Galactose-based aspirin prodrug was synthesized by using the α-d-glactopyranosyl bromide as glycosyl donor and aspirin as acceptor. The experimental method is simple and reproducible, has high yield and great practical value. The galactosylated aspirin prodrug was found to possess reduced cytotoxicity compared to aspirin, and selectively exhibited antiproliferative activity in the presence or in the absence of β-d-galactoside galactohydrolase with the approach of antibody-directed enzyme prodrug therapy (ADEPT) or the prodrug monotherapy (PMT).

Publisher URL: https://link.springer.com/article/10.1007/s00044-017-2094-4

DOI: 10.1007/s00044-017-2094-4

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