A series of chelants (3a–s) composed of a glucosyl tail, an amino acid side chain and a dithiocarbamate group were designed, synthesized, and evaluated. By co-administering with cisplatin, 3a–s were able to decrease the accumulation of platinum in the organs, maintain the accumulation of platinum in the tumor tissues, and increase the urinary and fecal platinum, as well as increasing the voided volume of the treated S180-bearing mice. Compared to S180-bearing mice treated with cisplatin alone, the co-administered mice lost no spleen, kidney, liver, brain and heart weights, lost less body weight, and showed no increase in tumor weight.