During the past 50 years, more than 100 000 compounds have been screened but only seven plant-derived anticancer drugs have received Food and Drug Administration (FDA) approval for clinical application. Identification of agents that are pharmacologically active against human cancer has depended largely on the screening of natural products and their analogs. Many anticancer drugs have been discovered fortuitously through random investigation of organisms; indeed, serendipity remains important in anticancer drug discovery. Although it is broadly accepted that cancers comprise an evolutionary microcosm, this idea has not been advanced to understand and control carcinogenic progression. Development of high throughput isolation of components from a crude natural product extract using highly automated separation techniques has enabled chemists to speed up the isolation, purification and characterization process. These modern techniques coupled with high throughput screening systems are expected to yield a lot more number of lead structures in the near future