A serious flaw of many chemotherapeutics employed now for the (post-surgery) treatment of malignant tumors is their high cytotoxicity against vital organs. In addition, tumor cells that survive chemotherapy often show pronounced drug resistance against a wide range of therapeutics. Recently, glycyrrhetinic acid derivatives derived from a cheap and easy-to-obtain natural product have attracted pharmacological interest. Many derivatives of glycyrrhetinic acid showed good to excellent cytotoxicity and inhibited the proliferation of a wide range of human tumor cells. They act predominantly by apoptosis, thus making them an interesting and even fascinating starting point for the development of selective, effective and safe antitumor active drugs.