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The aim of this study was to screen the phytochemicals from different solvent extracts of Memecylon umbellatum Burm F. by qualitative and quantitatively and to assess their free radical scavenging ability using various in vitro antioxidant assays. In this study, leaves of M. umbellatum was employed to isolate, identify and characterize bioactive compounds using different solvents of varying polarity such as hexane, chloroform, ethyl acetate, methanol and water. Among them, methanolic extract offered promising results in phytochemical parameters, hence the same alone was chosen to isolate the bioactive compounds. This study paved way for identification of new compounds which was selectively active against different human cancer which was predominant overall India as well as in the World. Further, cytotoxic and antiproliferative effect of purified bioactive compounds was tried on normal and human cancer cell lines. Based on the literature survey, it was clear that the plant influenced curative properties for human ailments.