competition assay and GLUT‐inhibitor‐mediated cytotoxicity analysis in a GLUT‐overexpressing human colorectal adenocarcinoma (HT29) cell line. The antitumor effect of the aminodeoxypyranoside‐conjugatedplatinum(II) complexes was found to depend significantly on the GLUT inhibitor, and the cellular uptake of the molecules was regulated by GLUT‐mediated transport. The results from this study demonstrate the