Copper (II) containing coordination complexes have attracted much attention for chemodynamic therapy (CDT) against cancer cells. In this study, the bimetallic nanobooster [Gd 2 Cu(L) 2 (H 2 O) 10 ]·6H 2 O was prepared by a solvothermal method based on tetrazole carboxylic acid ligand H 4 L [H 4 L = 3,3-di (1H-tetrazol-5-yl) pentanedioic acid]. It showed considerable cytotoxicity toward three kinds of human cancer cells (HeLa, HepG2, and HT29). The MTT assay showed that the IC 50 (half-maximal inhibitory concentration) of the complex NPs on HeLa cells (4.9 μg/ml) is superior to that of HepG2 (11.1 μg/ml) and HT29 (5.5 μg/ml). This result showed that [Gd 2 Cu(L) 2 (H 2 O) 10 ]·6H 2 O NPs can inhibit cell proliferation in vitro and may be potential candidates for chemodynamic therapy. In addition, the cytotoxicity was also confirmed by the trypan blue staining experiment. The results promise the great potential of Gd(III)-Cu(II) for CDT against cancer cells., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2022 Shi, Shen, Zhang, Tan, Shen, Zhong, Zhang, Gu and Shen.)