ABSTRACT: Cayratia pedata is an indigenous medicinal plant commonly known as Birdfoot Grapevine. The leaves of this plant have been used as a traditional medicine for the treatment of ulcers, diarrhea and inflammation. The crude extracts of the plant has anti-microbial, anti-ulcer, anti-inflammatory and anti-diarrheal properties. The present study reports on the bioactive principles obtained from Cayratia pedata through extraction, isolation and identification. The photochemical screened and quantitative analyses were done by biochemical tests. The preliminary analyses reveal the presence of tannins, flavonoids, terpenoids, alkaloids, carbohydrate, saponins, steroids, quinines, phenols, proteins, oils and fats, phytosterols, coumarins and phlobatannins. The ethanolic and aqueous extracts of Cayratiapedata Gagnep were found to possess moderate cytotoxic potential with reference to the standard drug Methotrexate against MCF-7 breast cancer cell line. Among the extracts, the ethanolic extract showed better activity than the aqueous extract when comparing with standard. .