This investigation describes the anticancer, antioxidant and antimicrobial properties of the extracts of Combretum rupicola, a native plant from Northeast of Brazil. Methanolic, ethyl acetate and chloroform extracts from leaves of C. rupicola were evaluated in relation to their potential in inhibiting the cell growth and cytotoxic properties against nine human cancer cell lines (MCF-7, NCI-ADR/RES, OVCAR-3, PC-3, HT-29, NCIH460, 786-O, UACC-62, K-562). In addition, antioxidant activity of these extracts was measured using DPPH as radical scavenging assay and the antimicrobial activities against nine pathogens were tested by agar diffusion method. Preliminary results showed that the this plant demonstrates to have moderate activity against bacteria but, on the other side, the extracts showed significant anticancer activitiesagainst four cell lines and the most significant activity was observed against MCF-7 (65.9 μg mL-1), highest inhibitory concentration IC50 0.22 μg mL-1 for antioxidant activity. 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