A four new penicillinate complexes were prepared through the chemical interactions of penicillin potassium salt (Pin) with YCl3, GeCl4, WCl6 and SiCl4 metal ions. These metal complexes were characterized using spectroscopic techniques (e.g. 1H-NMR, infrared, electronic UV-Vis) as well as elemental, conductivity, and magnetic measurements. The molar conductance values were highly, showing their electrolytic nature. The magnetic and electronic study strongly recommends the octahedral geometry of all penicillinate complexes. A monomeric structures of Pin complexes are proposed with octahedral coordinated metals ions. The metal ions are coordinated toward Pin as tridentate ligand through the amide and β-lactam carbonyls and a carboxylate group from penicillin. The in vitro antimicrobial activity of all the complexes, at concentrations in μg·mL-1, was screened against four bacterial pathogens, namely, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus, and two kinds of fungi Aspergillus flavus and Candida albicans showed better activity compared to parent drug and control drug. The anti-cancer inhibition of the tungsten(Ⅵ) complex was assessed against the human hepato cellular carcinoma (HepG-2) tumor cell line with IC50 value is 646 μg·mL-1.