Cancer is one of the most stern health dilemmas engulfing 7 million lives every year globally. It is group of more than 100 diseases. Conventional cancer therapies burdened the disease crippled patient with lethal side effects and are also very expensive. Therefore, the demand to use alternative approaches in treatment of cancer is escalating. Plants of earth are massive reservoir of bioactive compounds. Plant derived compounds such as protoapigenone, casticin, moursin, gypenosides VN5, kalopanaxsaponin A, sapindoside B7, maclekarpine C are foremost anticancer agents, due to their unique structure and sophisticated mechanism of action. The present review is aimed at compiling data on promising classes of bioactive compounds from medicinal plants and their anti cancer mechanism of action against different human carcinoma cell lines.