Cancer is one of the most dangerous health problems in the millennium and it is the third foremost human cause of death in the universe. Traditional cancer treatments face several disadvantages and cannot often afford adequate outcomes. It has been exhibited that the outcome of several therapies can be improved when associated with nanostructures. In addition, a modern tendency is being developed in cancer therapy to convert single-modal into multi-modal therapies with the help of existing various nanostructures. Among them, gold is the most successful nanostructure for biomedical applications due to its flexibility in preparation, stabilization, surface modifications, less cytotoxicity, and ease of bio-detection. In the past few decades, gold-based nanomaterials rule cancer treatment applications, currently, gold nanostructures were the leading nanomaterials for synergetic cancer therapies. In this review article, the synthesis, stabilization, and optical properties of gold nanostructures have been discussed. Then, the surface modifications and targeting mechanisms of gold nanomaterials will be described. Recent signs of progress in the application of gold nanomaterials for synergetic cancer therapies such as photodynamic and photo-thermal therapies in combination with other common interventions such as radiotherapy, chemotherapy, and will be reviewed. Also, a summary of the pharmacokinetics of gold nanostructures will be delivered. Finally, the challenges and outlooks of the gold nanostructures in the clinics for applications in cancer treatments are debated.