The planning, synthesis and antitumoral evaluation of Nα-(2,4-dinitrophenyl)-histidinethiosemicarbazide have been one field of research effort at the SintMed®. Exploiting the association between an amino acid scaffold and the thiosemicarbazide moiety, a new series of compounds was designed, and synthesised in order to investigate their biological activity. Once amino acids are a structural leitmotiv in the evolution, their incorporation in synthetic compounds represents a promising strategy toward the development of new antitumour drugs. A library of histidinethiosemicarbazide derivatives was prepared, and characterised through spectroscopic methods. Their biological activity are now under investigation, and the initial perspectives point to positive outcomes.