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Lung cancer, the most prevalent gender-independent tumor entity in both men and women, is among the leading cause of cancer-related deaths worldwide. Despite decades of effort in developing improved therapeutic strategies including immunotherapies and novel chemotherapeutic agents, only modest improvements in outcome and long-term survival of lung cancer patients have been achieved. Therefore, exploring new and exceptional sources for bioactive compounds that might serve as anti-cancer agents might be the key to improving lung cancer therapy. On account of diverse forms, cyanobacteria might serve as a potential source for compounds with potential therapeutic applicability against malignant disorders, including cancer. The assorted arrays of metabolic mechanisms synthesize a plethora of bioactive compounds with immense biological potential. These compounds have been proven to be effective against various cancer cell lines and xenograft animal models. The present review provides an overview of the most promising cyanobacteria-derived bioactive compounds proven to exhibit anti-cancer properties in in-vitro and in-vivo studies and highlights their applicability as potential therapeutic agents with a focus on their anti-lung cancer properties., (© 2022. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.)