Synthesis, Characterization and In Vitro Antitumor Activity of Glucosyl Ester Derivatives Containing Amino Acid Linker

Abstract

AbstractIn this present study, two series of glucosyl ester derivatives were synthesized by enzymatic acylation and their structures were characterized. The optimum condition was confirmed by experimental influence factors such as enzyme type, reaction time and temperature. The antitumor activity in vitro against three cancer cells including Human colon carcinoma (K562), Human hepatoma (HepG2) and human breast adenocarcinoma (MCF‐7) were evaluated using MTT methods. The results indicated that the glucosyl esters could significantly show high anticancer activity as their low IC50 values. Thereinto, methyl 6‐O‐(N‐dodecanoyl‐glycyl)‐α‐D‐glucosyl ester (16) and methyl 6‐O‐(N‐dodecanoyl‐valine acyl)‐α‐D‐glucosyl ester (20) showed higher inhibition effect to cancer cells than other compounds and control drug 5‐FU. The preliminary prediction of this type of compound had certain inhibitory effect on growth of tumor cells, and non‐toxic to normal cells. It is our propose to introduce many such novel amino acid sugar esters as antineoplastic drugs to be widely investigated.