• Lichens are a symbiotic relationship between two organisms an alga (Phycobiont) and a fungus (Mycobiont). Mycobiont predominates in the lichen thallus and provides its structure, form, as well as texture. Algae contribute to the thallus by providing nutrition. • The potential of lichens for medicinal use is to have a variety of bioactive anticancer compounds. • Synthesized lichen compounds may exhibit a range of bioactive constituents in response to their cytotoxic effects, including antioxidant, antibiotic, antimutagenic, antimicrobial, antibacterial, anti-inflammatory, antipyretic, inhibitory proteins, as well as endogenous plant growth impact. • Lichen derivatives have a wide range of anti-cancer effects against many forms of cancer cell types, like usnic acid, gyrophoric acid, and lechanoric acid. The potential of lichens for medicinal use is to have a variety of bioactive anticancer compounds. Several factors drive the issue of lichens as a usual substance of carcinoma chemicals for lichens. In a variety of climates which could be represented by extreme climatic variables, lichens can endure heat intensities, Ultraviolet rays, limited nutrient uptake, humidity, etc. Their results are obtained is due to the possible defence system they have towards severe change, simultaneously generating bioactive substances with distinctive attributes through different biosynthesis pathways. Synthesized lichen compounds may exhibit a range of bioactive constituents in response to their cytotoxic effects, including antioxidant, antibiotic, antimutagenic, antimicrobial, antibacterial, anti-inflammatory, antipyretic, inhibitory proteins, as well as endogenous plant growth impact. In addition, lichen derivatives have a wide range of anti-cancer effects against many forms of cancer cell types, like usnic acid, gyrophoric acid, and lechanoric acid. Furthermore, when functioning together through human cancer cells, lichens compounds can cause synergistic cytotoxic results. Anti-cancer stimulation of molecular lichen derivatives through the process of cytotoxicity by cellular processes and initiation of cell death and by modulation in immune activity, angiogenesis, or metabolism of energy. This review mainly focuses on the potential role of lichens' active constituents as beneficial moieties to exhibit anticancer activities with their molecular mechanism. [ABSTRACT FROM AUTHOR]