Background. Thiosemicarbazide derivates are considered potential compounds of the antitumor drugs, with a large spectrum of biological properties. The aim of the research was to reflect the actual progress in studies on thiosemicarbazide derivates, their complexes with metals and their mechanisms of activities. Material and methods. A systematic literature review was conducted for which the open electronic sources, through the PubMed web interface and HINARI collection of health literature were evaluated. Printed publications were found using the Universal Decimal Classification (UDC). Conclusions. Thiosemicarbazide derivates are chemical compounds of drugs with vast therapeutic potential. The improvement of their chemical structure could contribute to the development of new classes of drugs with better acceptability for in vivo experiments.