Synthesis and In Vitro Anti-tumor Evaluation of Novel Glycoconjugated SN38 Derivatives

Abstract Five types of novel glycoconjugated 7-ethyl-10-hydroxycamptothecin (SN38) derivatives were synthesized to evaluate their anti-tumor activity against HCT116 human colon cancer cells, and the results showed that all of them demonstrated potent anti-tumor activity. Notably, glucose and galactose conjugates exhibited the better anti-tumor activity, while the mannose and allose conjugates had slightly lower activity. Our findings suggested that the anti-tumor activity of glycoconjugated SN38 derivatives was affected by the type of modifying molecule used and the position of the modification. These findings could have implications for the development of novel anti-tumor agents targeting glucose transporters.