The benzimidazolium salts were synthesized by quaternization of 1-(4-tert-butylbenzyl)benzimidazole, with the corresponding benzyl bromides.The reactions were carried out in DMF at 70° for 48 h.Therefore, Ag2O and benzimidazolium salts were reacted in dichloromethane at room temperature under dark and Ag(I)-NHC complexes were obtained in very good yields.The Ru(II)-NHC complexes [(η6-p-cymene)RuCl2(1-R1-3-R2-2-Bzim)] (4a-d; 2-Bzim = 2-benzimidazolylidene, R1 = 4-tBuC6H4CH2; R2 = 4-MeC6H4CH2, 2,3,5,6-Me4C6HCH2, 4-tBuC6H4CH2, 3,5-Me2C6H3CH2) were synthesized via transmetalation reaction from the corresponding silver complexes [(1-R1-3-R2-2-Bzim)AgCl].The structures of the obtained compounds were characterized by different spectroscopic techniques such as 1H and 13C NMR, elemental anal., and m.p. detection.The lowest MICs values were obtained with the two complexes 4b,d.Enzymic inhibitory investigation against acetylcholinesterase (AChE) and tyrosinase (TyrE), showed that the two complexes and are the most potent inhibitors against (AChE) with an IC50 of 2.52 and 5.06 μg mL-1 resp., and against (TyrE) with an IC50 of 19.88 and 24.95 μg mL-1 resp.Screening of the selected N-Heterocyclic carbene (NHC) ligands and their resp. ruthenium (II) complexes against colon carcinoma cells lines (HCT-116) and hepatocellular carcinoma cells lines (HepG-2).Furthermore, compounds were showed weak cytotoxic action with IC50 ranging from 13.38 to 18.33 μg in human colon carcinoma cancer cell lines and from 14.36 to 18.45 μg in hepatocellular carcinoma cells lines.