The WHO says that annual cases of cancer will increase from 14 million in 2012 to 22 million in the next two decades. Cancer is the second cause of death in the world; in 2015, it caused 8.8 million deaths. On the other hand, it is necessary to consider that 70% of the total deaths due to this disease occur in developing countries, who have the least resources to acquire the drugs of choice for the treatment of this disease. Although there are treatments and these are effective, there are currently cases of resistance to drugs used to treat this disease, which has led to the search for new sources of drugs or compounds effective against the cancer being active; plants are the possible sources to achieve this. Cucurbitaceae is a family of plants widely distributed on the planet which has been used traditionally for the treatment of this disease and from they have been isolated different cucurbitanes. These compounds possess a wide biological activity, antidiabetic, anti-inflammatory, hepatoprotective, or cytotoxic and antitumoral effects. The aim of this review is to present 51 cucurbitacin compounds and 2 with different structures isolated from Cucurbitaceae plants with cytotoxic or antitumoral activity.