The article is a review of the data on synthesis and physiological activity of hybrid antioxidants. The introduction offers an explanation to the fact why, in some cases, it is necessary to add drug molecules with fragments responsible for various properties and aimed at various targets. A large group of hybrid antioxidants comprise stable nitroxyl radicals that behave as antioxidants in free-radical reactions of oxidation. Compounds of this type were synthesized extensively to form a group of antitumor agents. As a rule, the specific (antitumor) activity retained or even increased as compared with the initial compounds (without nitroxyl radicals); the toxicity decreased 5 to 10 times, which made it possible to apply the drug in considerably higher concentrations. There are reported data on nitroxyl derivatives of anthracycline antibiotics, antimetabolites, alkyl ting agents, and the recent results on platinum complexes with nitroxyl fragments. Much attention is given to hindered phenols with “buoyancy” properties, particularly, to biochemical effects, making them promising agents to treat Alzheimer’s disease.