Four DTPA and DOTA derivative ligands containing sulfonamide groups and their gadolinium complexes were prepared and characterized. Relaxivity studies showed that these gadolinium complexes possessed higher relaxation effectiveness than those of the corresponding ionic gadolinium complex Gd-DTPA and Gd-DOTA, respectively. In vitro cytotoxicity assay demonstrated that these gadolinium complexes have low cytotoxicity to the human liver cells (L-02). Magnetic resonance imaging (MRI) and experimental data of biodistribution in mice indicated that these gadolinium complexes containing sulfonamide groups could be used as the potential MRI contrast agents for Hepatoma (H22) and Ehrlich ascites carcinoma (EAC) in mice and specific organs such as the liver and could be mostly excreted by the kidneys.