Treatment of cancer is a challenge. Chemotherapy agents used for its treatment damage healthy cells; the immune system is also disabled following treatment with the latest chemotherapy agents. Chemotherapy agents used also weaken the immune system, leaving the human body vulnerable, the patient may die, and serious difficulties faced in its treatment. We need safe chemotherapeutic agents which target cancer cells without damaging healthy cells. Ancient Egyptians believed that mushrooms were "agents of immortality". Among Pharaohs, only the royal family could eat mushrooms. Mycochemistry of Ganoderma species has shown these could be used against cancer treatment. Cytotoxic activity-guided isolations have been done to find the potential drug. Phytochemical studies are done to find the immunomodulatory, antiviral, anti-inflammatory, α-glucosidase inhibitory, acetyl-cholinesterase and butyrylcholinesterase inhibitory, and antibacterial compounds. G. lucidum has been used as immunomodulator and antitumor agent. It is excellent source of bioactive mycochemicals. Other Ganoderma species are too studied for the potential to be used. The compounds (1-463) isolated from 17 Ganoderma species in the last two decades have been evaluated along with their anticancer and related biological activities. Meanwhile, terpenoids, steroids, phenolics, and alkaloids, indicating biological activity related to cancer from 17 Ganoderma species, are reported herein. © Springer Nature Switzerland AG 2021. All rights reserved.