Camptothecins are a class of highly potent and selective topoisomerase I inhibitors, derived from the bark and leaves of the Camptotheca acuminata tree. These natural products have shown significant therapeutic potential in the treatment of various cancers due to their ability to induce DNA damage and cell cycle arrest. Structurally, camptothecins consist of a core 10-deacetyllignan moiety linked to an alkaloid group, which is responsible for their pharmacological activities. Camptothecin derivatives, such as topotecan and irinotecan, have been extensively studied and are approved by regulatory agencies worldwide for the treatment of cancers including ovarian, small cell lung, and colorectal cancer. In addition to their antitumor effects, camptothecins also exhibit anti-inflammatory properties, making them promising candidates for further exploration in diverse therapeutic areas. The mechanism of action of camptothecins involves the formation of a complex with topoisomerase I and DNA, leading to the generation of single-strand breaks in DNA. This process can ultimately result in cell death through apoptosis or necrosis, depending on the extent of DNA damage. Due to their potent cytotoxicity and selective nature, camptothecins represent an important class of anticancer agents with broad therapeutic applications.