7-Ethyl-10-hydroxycamptothecin (SN38), a highly potent metabolite of irinotecan, has an anticancer efficacy 100-1000 folds more than irinotecan . However, the clinical application of SN38 has been limited due to the very narrow therapeutic window and poor water solubility. Herein, we report the SN38-glucose conjugates (Glu-SN38) that can target cancer cells due to their selective uptake glucose transporters, which are overexpressed in most cancers. The antiproliferative activities against human cancer cell lines and normal cells of Glu-SN38 were investigated. One of the conjugates named showed high potency and selectivity against human colorectal cancer cell line HCT116. Furthermore, remarkably inhibited the growth of HCT116 . These results suggested that could be a promising drug candidate for treating colorectal cancer.