Abstract
This paper presents a brief historic of bioactive natural products against cancer. Some aspects of current research in pharmacological and biochemical profiling of lead compounds obtained from traditional medicinal plants are herein presented. Emphasize some important natural anticancer agents and general chemotherapeutic approaches, including mutagenic investigation. The very efficient Amazonian Euphorbiaceae medicinal plant Croton cajucara, which is the source of the bioactive clerodane trans-dehydrocrotonin, is focused. The chemotherapeutic potential of this substance should be explored in order to achieve new anticancer drugs. The advantage of its incorporation into drug delivery systems is also explored.