Kopsia singapurensis Ridl. is one of the species of the genus Kopsia, also called white kopsia or locally known as ‘selada’ which about 18 species were distributed in Malaysia. This species is endemic only to Peninsular Malaysia and Singapore. This plant is known to produce a large number of biologically active compounds. In the present study, six known compounds were obtained from the hexane crude extract from the leave and bark of Kopsia singapurensis and identified as: lupeol 1, lupeol acetate 2, β-amyrin 3 β-amyrin acetate 4, β-amyrone 5 and stigmasterol 6. The structures of these compounds were elucidated by combination of various spectroscopic methods such as MS, UV, IR, 1D and 2D NMR, involving also comparison with data from the literature. All the isolated compounds exhibited cytotoxic effects against MCF-7 cell line, compound 6 was the most active compared to the rest of the compounds in the cytotoxic activity with IC50= 14.5µg/mL, while all tested compounds showed no significant on antibacterial (gram-positive bacteria, Bacillus cereus) and antioxidant activity using the DPPH method.