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Nowadays, one of the most important research directions that concerns the scientific world is to exploit the earth’s resources in a sustainable way. Considering the increasing interest in finding new sources of bioactive molecules and functional products, many research studies focused their interest on demonstrating the sustainability of exploiting marine macroalgal biomass as feedstock for wastewater treatment and natural fertilizer, conversion into green biofuels, active ingredients in pharmaceutical and nutraceutical products, or even for the production of functional ingredients and integration in the human food chain. The objective of the present paper was to provide an overview on the recent progress in the exploitation of different macroalgae species as a source of bioactive compounds, mainly emphasizing the latter published data regarding their potential bioactivities, health benefits, and industrial applications.