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One of the main problems that appear in cancer chemotherapy is the toxicity of the established drugs. However, naturally, derived products have been proven to be safe and effective in the treatment and management of cancers. Hence, in the current trend, most researchers are doing their research on bio-based natural products to treat cancer. Many naturally-derived products or their analogs have been identified as potent anti-cancer agents and similarly, the anti-cancer potential of various bio-compounds is being identified day by day. Considering this data on the increasing importance of bio-compounds, we have also attempted to study the efficacy of Hispolon, Limonene, and a combination of Doxorubicin in the treatment of colon cancer. This book mainly focused on the investigation of the combinatorial anti-cancer effect of Doxorubicin, Hispolon, and D-Limonene against colorectal cancer cell lines, which was determined by different cell-based and Molecular based assays.