A series of new N-[(3-ferrocenyl-1-phenylpyrazol-4-yl)methyl] α-amino acids were prepared and characterized by a range of spectroscopic techniques and cyclic voltammetry. The in vitro antitumor activity of all synthesized compounds was investigated against cervix adenocarcinoma HeLa, melanoma Fem-x and myelogenous leukemia K562 cell lines using the MTT method. Tryptophan derivative 1l exhibited the highest cytotoxic activity in the cell growth inhibition of all three types of cell lines.