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Platinum-based anticancer drugs have been successfully applied in clinical, which greatly promoted the development of metal-based medicinal chemistry. Currently, seeking for metal-based drugs with new action mechanism has become one of the hot topics in medicinal chemistry. Herein, we review the research progress on antitumor and antibacterial activity of 8-hydroxyquinoline and its derivatives’ metal complexes. From synthesis, structure, activity, action mechanism and structure-activity relationship, the recent progress of 8-hydroxyquinoline and its derivatives’ metal complexes with antitumor activity have been summarized. Also, the advances of 8-hydroxyquinoline and its derivatives’ antibacterial metal complexes have been reviewed. Basing the facts mentioned-above, we find some active groups and some trends of halo-substituted effect, which may afford important references for designing and developing new antitumor and antibacterial 8-hydroxyquinoline and its derivatives’ metal-based drugs.