Cancer is a complex disease that transforms a normal cell into a malignant cell by disturbing different molecular mechanisms. Lately, plant‐derived bioactive products have gained prominent attention to serve as anti‐cancer agents. These natural anti‐neoplastic agents are believed to act as alternatives for the synthetic drugs or could be used to enhance the prospect of other drugs in reducing their dose, thus limiting their possible toxic effects. They could also counterbalance the other anti‐cancer drug‐induced adverse effects. Among natural plant‐derived products, coffee has been reported for its significant anti‐carcinogenic effects in the scientific literature. This article aims to highlight the anti‐cancer potential of different coffee components viz. caffeic acid, chlorogenic acids, caffeine (1,3,7‐trimethylxanthine), cafestol, ferulic acid, and kahweol together in a single article. Based on our article, it is quite clear that these bioactive components have important therapeutic potentials against cancerous cells. However, the lack of clinical data negates their use in humans. Therefore, more research is recommended to achieve the desired pharmaceutical value. We also implore assessing their safety and possible adverse effects prior to their progress into clinical trials. © 2018 BioFactors, 44(4):315–326, 2018