Our work is focused on multi-targeted metal complexes as potential therapeutic agents in cancer therapy because of their unique characteristics, such as redox activity, variable coordination modes, and reactivity toward the organic substrate. Their noteworthy properties have attracted much attention in the design and synthesis of metal complexes that specifically bind to the biomolecular target without hampering normal metabolic conditions, ultimately leading to cancer cell death. We are using Pt, Ir, Au, and Ru metals for targeting cancer cells. One of the major challenges in cancer therapy is the selective targeting of cancer cells to avoid irreversible damage to normal cells. A prodrug strategy could be the most impressive solution to solve this problem. We are very much delighted to work on prodrug therapy including metal complexes that work on tumor-microenvironment sensitive and specific cancer biomarkers activation conditions. We are also working on Photodynamic therapy which is a non-invasive treatment for cancer therapy. To avoid damage through irradiation during PDT to normal cells we are also developing smart photosensitizers which could only get activated by certain tumor-specific reaction conditions and release an elevated amount of reactive oxygen species. This could provide a new arch in designing anticancer drugs to avoid obstacles caused by conventional chemotherapeutics.