Ten compounds were isolated from the n-butanol extract of Pittosporum eugenioides leaves and evaluated for their antioxidant properties and cytotoxic activity. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical using ascorbic acid as standard antioxidant and total antioxidant capacity (TAC) (phosphomolybdenum assay). The overall antioxidant activity of compounds 1, 2, 3 and 4 showed the strongest one among the tested compounds with values of 1.28±0.97, 3.21±0.24, 5.40±0.08 and 7.09±0.07 μg/ml, respectively compared to the SC50 value of the positive ascorbic acid control was 7.9±0.78 μg/ml. Also, these compounds were evaluated for their cytotoxic activity against brine shrimp (Artemia salina L.). The LC50 values ranged between 11 to 25 μg/ml, for the compounds 1-10. The present study reveals that the selected plants would exert several beneficial effects by virtue of their antioxidant and cytotoxic activity and could be harnessed as drug formulation.