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The imbalance expressing of Cu/Zn superoxide dismutase (SOD1) in vivo will cause intracellular oxygen reduction signal to disorder, which leads to cell proliferation, tumorigensis and damage motorneurons.We designed and synthesized Cu(Ⅱ) chelating ligands to distinguishingly bind with the active site of Cu in SOD1, as a result, the SOD1 lost its activity and then the relative concentrations of intracellular ROS was regulated.