In order to establish the medicinal properties as anticancer agents from the non-edible of cocoa plant parts, the studies on fresh of non-edible cocoa plant parts such as cocoa leaf (CL), cocoa bark (CB), cocoa husk (CH), cocoa shell unfermented (CSUF), cocoa shell fermented (CSF), cocoa root (CR), cocoa cherelle (CC) & cocoa pith (CP) were performed by extracting in methanol solvent, screening against various type of cancer cell lines, purified using bioassay guided fractionation and identified active compounds using gas chromatography-mass spectrometry (GCMS). Results revealed that the cocoa leaf extract presented the highest antiproliferative activity against breast cancer cell line (MCF-7) with IC50 value was 41.43 ± 3.26 μg/ml and selected for further purification using bioassay guided fractionation. The hexane partitioned fraction of cocoa leaf showed the highest anticancer activity with IC50 value about 66.7 ± 7.95 μg/ml. Hexane partitioned fraction was further purified using flash column chromatography and divided into 3 steps such as fractionation-1, fractionation-2 and fractionation-3. Sample fraction II/F7 from fractionation-2 was selected for chemical characterization using GC-MS due to the highest anticancer cancer activity with IC50 value was 6.36 ± 0.71 μg/ml and generated 10 major active compounds with synergistic effect against MCF-7. Nine compounds were known compounds and one compound was unknown compound. Theobroma cacao is still an underutilized plant and its bean has been used traditionally as source of food and medicine. The consumption of cocoa leaf as non-edible part could provide health benefits especially to treat human cancer in the future.