Introduction: Tumor diseases are one of the leading diseases of modern society and occur in all age groups. Their development takes place in three stages: initiation, promotion and progression. In the last few years, with the progress of medicine, new potential compounds have been discovered that would have anti-inflammatory and anti-tumor effects. Quinoline and coumarin derivatives and their rhenium (I) carbonyl complexes have been discovered as compounds that have a diverse structure, each of which has its own importance in the production of drugs. The aim of the research: (1) to examine the antitumor activity of quinoline and coumarin ligands and their complexes with rhenium on a panel of tumor cells; (2) to examine the antiinflammatory activity of quinoline and coumarin ligands and their complexes with rhenium by determining nitric oxide and malonylaldehyde with RAW264.7-induced liposaccharides; (3) to determine the antioxidant capacity of quinoline and coumarin ligands and their complexes with rhenium Materials and methods: Antiproliferative activity was determined by the MTT test on cell lines: MRC-5 (human fibroblasts isolated from fetal lungs), human cervical cancer cells - HeLa, human colon adenocarcinoma cells (Caco-2), acute monocytic leukemia cells ( THP-1), lymphoma 8 Hut-78 T-cells), acute lymphoblastic leukemia cells (CCRF-CEM) and mouse macrophage cell culture RAW 264.7). The antioxidant capacity was determined by the ABTS method. NO concentrations were determined by the Griess test and lipid peroxidation by the TBARS test Results: Ligands 1 and 2 and their complexes (Re-1 and Re-2) inhibit the growth of leukemia and lymphoma cells more strongly than cancer cells. The Caco-2 cell line showed the highest sensitivity to the test compounds. Complexes with rhenium showed stronger antiproliferative effects compared to the effects of the ligands individually. The tested compounds have a lower antioxidant capacity compared to trolox and esculetin and inhibit the formation of nitric oxide in LPS-stimulated RAW264.7 macrophages. Tested compounds have no effect on lipid peroxidation in LPS-stimulated RAW264.7 macrophages. 9. SUMMARY 31 Conclusion: It is necessary to carry out further research in the direction of clarifying the mechanism of action of the tested compounds, considering the observed selective effects on the growth of leukemia and lymphoma cells.