Acmella calva (DC) R. K. Jansen is a medicinal herb widely used by different communities as a traditional cuisine and food ingredient. Different parts of this toothache plant are used as medicine to treat stomatitis, mouth ulcers, and characteristically for toothaches. The current investigation was carried out in search of bioactive compounds of plant parts (stem, leaves, and inflorescence) extracted in ethanol. The elements identified were specifically Caryophyllene 13.45%, Neophytadiene 21.08%, and N-Isobutyl-(2E,4Z,8Z,10E) dodecatetraenamide 25.30 % and peak area was found as a major compound in stem, leaf, and inflorescence respectively by GC-MS. The anticancer activity was evaluated against MCF-7 Human breast cancer cell line at the doses of 10 to 100 μg/ml extract for stem, leaves, and inflorescence. A significant reduction in mobility of the cell line was demonstrated by the stem, leaves, and inflorescence as an exposure of MCF7. The bioactive compounds collectively act on cancer cells to exert significant cytotoxicity and apoptotic activity on the MCF-7 cell line. It was drastically reduce the mobility of cells, elucidating A. calva as a promising agent against MCF7 that can be further purified and utilized in anticancer studies.