A novel, dinuclear and dissolvable palladium(II) complex of [{Pd(en)Cl}(2)(mu-p-ph-da)](NO3)(2), where en is ethylenediamine and p-ph-da is 1,4-phenylenediamine, was synthesized by the reaction between [Pd(en)(dmf)Cl](NO3) (dmf = dimethyl formamide) and p-ph-da in the molar ratio of 2:1. The structure and formulation of the complex were also proposed on the bases of elemental analysis, conductivity measurements, and spectral (FT-IR, UV-Vis, and NMR (H-1 and D2O exchange)) data. The complex was screened for its antitumor activity against MOLT-4 have shown a significant decrease in viability after 24 h which was also dose-dependent. Rich CT-DNA and BSA interaction studies including absorption, fluorescence, thermodynamic, energy transfer, electrophoresis, cyclic voltammetry, and circular dichroism revealed that hydrogen-binding, van der Waals, and electrostatic attractions are different binding forces for the complex interacting with the above biomacromolecules. Likewise, molecular docking simulation supports the above experimental conclusions.