Objectives: The ocean is a huge ecosystem with diverse marine life. Scientists have found a large number of natural products with unique structural features and excellent biological activity from these organisms. Marine-derived sulphur-containing alkaloids are a significant family of nat-ural products with diverse structures and bioactivities. In this paper, the chemical and biological diversity of 972 sulfur-containing alkaloids derived from marine organisms reported from 1982 to 2022 were reviewed, and the structure-activity relationship was briefly analyzed, in order to pro-vide reference for the discovery, synthesis, biological activity research and drug development of such compounds.Key findings: A total of 972 marine-derived sulphur-containing alkaloids have been collected. Among them, 80.36% of sulphur-containing alkaloids are from marine sponges, fungi, tunicates and bacteria. Moreover, cytotoxicity is their most significant property, About 1/3 sulphur -containing organisms are reported to be cytotoxic. Aming them, discorhabdins, curacins, tanjun-gides, leptosins, and latrunculins exhibit better cytotoxicity. In addition, the structure-activity rela-tionships of the cytotoxicity of these compounds have been summarized for further investigation. Summary: In this paper, the chemical and bioactivity diversity of marine-derived sulphur -containing alkaloids were reviewed, which are a significant family of natural products with diverse structures and bioactivities. 972 sulphur-containing alkaloids were obtained from marine algae, sponges, cnidarians, tunicates, echinoderms, molluscs, bryozoans, dinoflagellates, cyanobacteria, bacteria and fungi, which possessed a wide spectrum of pharmacology including cytotoxicity, anti-bacterial, antifungal, antimitotic, antiviral, and other activities.& COPY; 2023 The Author(s). Published by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).