In recent years, metallodrugs have been playing an important role, showing to be more efficient in the treatment of several diseases, such as cancer. Indeed, it is important to synthesize novel molecules to be used as more effective agents against cancer. In the present paper, the synthesis of two new molecules belonging to Casiopeínas(®) is reported. These compounds present a β(2)-aminoacidate derivative as the secondary ligand. The novel metal complexes were characterized by high-resolution mass spectrometry, FT-IR, UV-Vis, EPR, effective magnetic moment and cyclic voltammetry measurements, and single crystal X-ray diffraction analysis. Furthermore, these compounds were evaluated in vitro against the cancer lines MCF-7 (breast cancer) and A549 (lung cancer).