The ocean is a valuable natural resource that contains numerous biologically active compounds with various bioactivities. The marine environment comprises unexplored sources that can be utilized to isolate novel compounds with bioactive properties. Marine cyanobacteria are an excellent source of bioactive compounds that have applications in human health, biofuel, cosmetics, and bioremediation. These cyanobacteria exhibit bioactive properties such as anti-inflammatory, anti-cancer, anti-bacterial, anti-parasitic, anti-diabetic, anti-viral, antioxidant, anti-aging, and anti-obesity effects, making them promising candidates for drug development. In recent decades, researchers have focused on isolating novel bioactive compounds from different marine cyanobacteria species for the development of therapeutics for various diseases that affect human health. This review provides an update on recent studies that explore the bioactive properties of marine cyanobacteria, with a particular focus on their potential use in human health applications.