Pyrazine-bipyrazole-based µ-oxo bridged dinuclear Au(III) complexes were synthesized and characterized by various spectrometric ( 1 H-NMR,  13 C (APT) NMR, FT-IR, Mass spectrometry) and analytical techniques (elemental analysis and conductance measurement). The evaluation of DNA binding activity by UV-Vis absorption spectra and viscosity measurement demonstrated that all the compounds intercalate in between the stacks of DNA base pair and the binding constant values were observed in the range of 5.4 × 10 4 -2.17 × 10 5  M -1 . The molecular docking study also supports the intercalation mode of binding. The anti-proliferation activity of complexes on A549 (Lung adenocarcinoma) cells by MTT assay demonstrated IC 50  values in the range of 47.46 -298.12 μg/mL. The genotoxicity of compounds was checked by smearing observed in the DNA of S. pombe cell under the influence of complexes. The in vivo cytotoxicity of compounds against brine shrimp demonstrated the LC 50  values in the range of 4.59-27.22 μg/mL. The promising results of the Au(III) complexes received significant attention and make them suitable for the new metallodrugs after the detailed mechanistic biological study.