Incorporation of biologically-active ligands into a metal (organo-metallic complexes) offers much scope for the design of novel therapeutic agents with enhanced targeted activity and new mode of action. Several ruthenium complexes have been reported to be promising biological activities. Here, some novel organometallic ruthenium (Ru) complexes, bearing thiosemicarbazone moieties were synthesized and screened for various pharmacological activities. It has been identified that the new Ru(II)-arene complexes demonstrating the validity of such an approach to the design of novel drugs in near future.