Within this dissertation, the total synthesis of marinoaziridine B, the methylated derivative of marinoaziridine A and their structural derivatives was developed for the first time. The structures of marinoaziridines A and B were optimized by quantum-chemical calculations using the DFT functional B3LYP with the use of the 6-311++G(d,p) basis set, and the solvation effect (chloroform) on the equilibrium of the tautomeric pairs of quinolin-2(1H)-on was examined. An enantioselective method was developed for the separation of enantiomers of marinoepoxide and marinoaziridine on polysaccharide chiral stationary phases based on amylose and cellulose derivatives using high performance liquid chromatography and supercritical fluid chromatography. The absolute configuration was successfully determined using computational and chiroptical methods (electronic circular dichroism, ECD and vibrational circular dichroism, VCD). Biological tests of marinoaziridine and selected derivatives were performed on three cell lines (MCF-7 breast cancer, H-460 lung cancer and HEK293T embryonic kidney) and on bacterial cultures of Escherichia Coli and Staphylococcus aureus. Toxicological tests were performed using a test on zebrafish embryos.