Series of organoruthenium complexes and their nano biocomposites were prepared and analyzed by various spectral analyzed techniques like infrared (IR), UV-Vis, 1 H-nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR) spectroscopy, and high-resolution mass spectrometry (HR-MS). The redox properties of organoruthenium complexes were studied by cyclic voltammogram. UV-Vis and fluorescence spectroscopy employed to study the binding affinity of Ru (III) complexes with CT-DNA and serum albumin (bovine serum albumin [BSA]). From the K sv and K b values, the interaction between BSA and organoruthenium complexes confirmed the mechanism of binding as static quenching. Scanning electron microscopic (SEM) studies validated the formation of new hybrid organometallic proteomics (P1-P4), while binding of the complexes with protein (BSA). A comparative cytotoxic profile of organoruthenium complexes and their nano biocomposites were evaluated. The results revealed the higher anticancer activity of nano biocomposites than their parent organoruthenium derivatives.