Lamellarins are a group of marine active pyrrole alkaloids isolated from prosobranch mollusks. So far, over 40 lamellarins have been isolated and identified. As the best known member in this series, lamellarin D (LMD) exhibits a significant cytotoxicity against a large panel of cancer cell lines and is a potential non-CPT (camptothecin) topoisomerase 1 poison. It affects cell cycle and acts on cancer cell mitochondria to induce apoptosia. The recent progress in LMD and its derivatives is reviewed in this paper based upon authors’ work. The synthesis of LMD and its derivatives is emphatically introduced, including two major methods (synthesizing the core pyrrole ring as well as starting from pyrrole ring). Furthermore, some promising research trends are proposed.

Key words: alkaloid, cytotoxicity, chemical synthesis, topoisomerase 1 inhibitor, lamellarin D