Аннотация:Recently the interest in [1,4]-benzodiazepine derivatives as components of potential anticancer drugs has increased significantly. This is due largely to the ability to form the antibody- drug conjugates for the targeted drug delivery [1].A number of derivatives of [1,4]-benzodiazepines with a positive computer forecast was synthesised by the four-component Ugi reaction. All compounds contain reactive functional groups which are suitable for further chemical modification in order to obtain the original biologically active compounds. Structures of all obtained compounds have been confirmed by the spectral analysis.A quantitative forecast of the profiles of antitarget interaction of chemical compounds was carried out using the GUSAR software (http://www.way2drug.com/gusar/antitargets.html). In this work materials collected by PhD Apryshko G.N. were also used. In the preclinical study of the compounds, the MTT-test on 9 lines of tumor cells and transplanted tumors of mice from the bank of tumor strains of N. N. Blokhin Russian Cancer Research Center of Ministry of Health of Russia (P-388 lymphocytic leukemia and epidermoid lung carcinoma Lewis LLC) were used. The obtained results demonstrate the activity of the synthesized [1,4]-benzodiazepines with the prospect for further research.