Several members of species Caesalpinia (Caesalpiniaceae) are being used traditionally for a wide variety of ethanomedicinal properties. C. sappan is one amoung them found in India.A decoction of the heartwood is commonly used in Kerala, India for its antithirst, blood purifying, antidiabetic,improvement of complexion and for several other properties.The phytoconstiuents isolated and charactersied from Caesalpinia sappa can be categorized under flavonoids and sterols. The chemical constituents isolated from different extracts of heartwood namely, Protosappanin A, B & C, Brazilein, Brazilin and aromatic alcoholic compound of Brazilin, Campesterol and Stigmosterol.further these extracts were screened for cytotoxicity studies,from which ethanolic extract and ethyl acetate fraction exhibited the most cytotoxicity activity against all the three cancerous lines viz; HEP-2, HeLa and A-549 with CTC50. The petroleum ether fractions were potentially cytotoxic to HEP-2 and A-549 cells with CTC50. From overall,it is evident that, C. sappan heartwood is in-vivo anti-tumor activity there by justifying their use in the traditional system of medicine.