Thiosemicarbazide derivatives are widely used in medicine in treating various types of diseases. All of them have a wide range of reactive atoms and form with metal ions biologically active coordination compounds with a various composition and properties. It was determined that in many cases biological activity of these compounds consists with their structure. Therefore, accumulation and systematization of the experimental data on synthesis, physicochemical researching of their composition and structure are of both scientific and practical interest. The aim of this work is the synthesis, determination of the composition, structure, antitumor and antimicrobial activity of the coordination compounds of cobalt, nickel, copper and zinc with salicylaldehyde and 2-hydroxynaphthalene-1-carbaldehyde 4-(pyrid-2-yl)thiosemicarbazones and their derivatives (H2L1-10). The experiments showed that chlorides of stated above metals react with thiosemicarbazones HL1-10 in ethanol solution in 1:1 or 1:2 molar ratio forming fine-crystalline compounds of different colors and composition. The composition of these compounds was determined using elemental analysis: M(HL1-10)Cl (M = Ni, Cu, Zn); Co(HL1-10)2Cl. The structure of the synthesized compounds was determined on the basis of data from NMR spectroscopy (1H and 13C), IR spectroscopy, magnetochemical research, and X-ray diffraction analysis for some of them. The synthesized thiosemicarbazones HL1-10 behave as tridentate ligands with O, N, S set of donor atoms. Bacteriostatic and bactericidal activity of these compounds was determined on a series of standard strains of gram-positive and gram-negative microorganisms. It was found that these compounds show selective antimicrobial activity for all of the tested strains in the range of concentration 0.005-10.0mg/ml. The minimal bactericidal concentration significantly depends on the nature of the central atom in the composition of homotypic complexes in the following way: Cu> Zn>Co≈Ni. Moreover, the sinthisezed coordination compounds inhibid the human promyelocytic leukemia HL-60 cells’ proliferation up to 100% in the range of concentration 10-5 -10-6 mol/l.