In the search for chemopreventive agents for cancer many natural products have been identified. Among them extensive experimental studies have been made on protease inhibitors which not only occur naturally in many plant products, but have also been synthesized in the laboratory. Many of these studies revealed the fact that protease inhibitors are able to prevent carcinogenesis and tumour promotion. A review of the reports available to date suggests that protease inhibitors are potential chemopreventive agents although their biological role and mechanism of action are not very clear.