**Abstract**

Potent biomolecules from natural products from plants, animals, and minerals are the fundamental basis of the ailment of mankind. *Capsicum* or red pepper plants were grouped under the kingdom Plantae and family Solanaceae. It is used widely throughout the world in foods for their pungent flavor and aroma, and to prolong food spoilage. This chapter presents a frame of a concise compilation of the anticancer and cytotoxic potentials of *Capsicum*, its analogs, and related compounds. Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide) is the most predominant and naturally occurring alkaloid from the *Capsicum* species. It also details the anticancer efficacy of capsaicin and its analogs like capsaicinoids and capsiates which possess antioxidants and targets multiple signaling pathways, ontogenesis, and tumor-suppressor genes in various types of cancer models. Capsaicin is a major ingredient and has been linked to suppression of growth in various cancer cells. The data available strongly indicate the significant anticancer benefits of capsaicin and its potent analog molecules. It shows a significant effect on cancer cell proliferation, apoptosis, cancer cell surveillance, growth arrest, and metastasis. This chapter also predominantly focuses on the combinational use of capsaicin with other natural dietary compounds as a measure of synergistic anticancer activities.

**Keywords:** *Capsicum*, capsaicin, apoptosis, angiogenesis, metastasis, anticancer
