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Cancer is a leading cause of deaths worldwide. The current search for alternative drugs is imperative. Medicinal plants are the most promising source of new anticancer agents. This study evaluated the phytochemical composition, and anti-proliferative activity of Methanol-Dichloromethane (1:1) extracts from the leaves, stem and fruits of Oxygonum sinuatum. Phytochemicals screening was done using standard procedures which were based on color change and/or precipitation. The MTT assay was used to test for the anti-proliferative activity of the plant extracts on selected cancer cell lines. In addition, normal Vero cells were used. 5-flourouracil was used as the standard drug. Results from this study revealed that stem, leaves and fruits extracts contained alkaloids, glycosides, saponins, tannins, flavonoids, terpenoids, steroids and phenols. The leaves, stem and fruits extracts showed moderate anti-proliferative activity on 4T1, Hcc 1395, 22Rv1 and DU145 with the best activity been registered by fruits extract on 4T1 cell line; 35.841±3.549µg/ml. The fruit extract showed no activity on DU145 cell line. The leaves and fruit extract showed no toxicity to Vero normal cells (CC50 >1000µg/ml) however, the stem extract was toxic to Vero cell, CC50 413.733±21.022 µg/ml. The highest selectivity index was registered by fruit extract on 4T1; SI=27.90. The leaves and stem extracts also showed high selectivity (SI >3) on 22Rv1 and DU145 respectively. The anti-proliferative activity of Oxygonum sinuatum on the selected cancer cell lines can be attributed to the phytochemical compounds present in the plant extracts.