Gold nanobioconjugates have emerged as a promising tool for targeted cancer therapy. Cancer is a complex and heterogeneous disease, and conventional chemotherapy often lacks selectivity and causes severe side effects due to the nonspecific targeting of normal cells along with cancerous ones. Therefore, there is an urgent need to develop targeted drug delivery systems that can deliver therapeutic agents specifically to cancer cells, thus minimizing toxicity to normal tissues. Gold nanobioconjugates have unique physicochemical properties such as small size, high surface area-to-volume ratio, and optical properties that make them an excellent platform for targeted drug delivery. The design, synthesis, and characterization of gold nanobioconjugates for targeted delivery of drugs and nucleic acids in ovarian cancer and noninvasive bioimaging are the focus of this review. The use of nanoparticles as drug delivery systems requires biocompatibility, and gold nanobioconjugates have been shown to be biocompatible in vitro and in vivo. Furthermore, the surface of gold nanoparticles can be modified with different ligands such as peptides, antibodies, and aptamers to achieve tumor targeting. The cellular uptake and intracellular delivery of gold nanobioconjugates in cancer cells have been extensively studied. Biofunctionalization of the nanoparticle surface with targeting ligands improves their uptake by cancer cells and reduces nonspecific uptake by normal cells. The efficacy of gold nanobioconjugates in delivering different types of therapeutics such as drugs, nucleic acids (siRNA, miRNA, and CRISPR/Cas9), and immunotherapeutics has been investigated in various preclinical studies. Noninvasive bioimaging is a crucial aspect of cancer diagnosis and treatment. Gold nanobioconjugates have unique optical properties that can be exploited for bioimaging. Different imaging modalities such as surface plasmon resonance, fluorescence imaging, positron emission tomography, magnetic resonance imaging, optical imaging, photoacoustic imaging, and computed tomography have been used to track the biodistribution, clearance, and immune response of gold nanobioconjugates. The toxicity, pharmacokinetics, and pharmacodynamics of gold nanobioconjugates have also been investigated in preclinical studies. It is essential to understand the toxicity of these nanoparticles to minimize adverse effects in patients. The immune response to gold nanobioconjugates and their potential for personalized medicine are other areas of interest. In conclusion, gold nanobioconjugates offer an exciting avenue for targeted cancer therapy, and their potential for clinical translation is enormous. Further research is required to fully understand the potential of these nanoparticles in cancer therapy and their impact on human health.