Two metal complexes formulated as [Zn(L) 2 ] 2 ·H 2 O (1) and [Bi(L)(NO 3 ) 2 (CH 3 OH)] (2), where HL=2-acetylpyrazine N(4)-phenylthiosemicarbazone, have been synthesized and characterized by elemental analysis, IR, MS, NMR and single-crystal X-ray diffraction studies. Biological studies, carried out in vitro against selected bacteria and the K562 leukemia cell lines, respectively, have shown that the free ligand and its two complexes may be endowed with important biological properties, especially HL with MIC=3.90μg/mL against Pseudomonas aeruginosa, the zinc(II) complex 1 with IC 50 =1.0μM against K562 leukemia cell lines, respectively. The compounds HL and 1 may exert their cytotoxicity activity via induced loss of mitochondria membrane potential (MMP).