As a result of their powerful biomedical potentialities, and considering their limited natural quantities, lamellarins have attracted immensely worldwide organic chemists and pharmacists to scale up their availability though economic, effective, and practical synthetic strategies. Three elegant synesthetic tactics including pyrrole ring functionalization, cycloaddition/condensation reactions incooperating isoquinoline scaffold and coumarin derivatives approach were able to not only totally synthesising natural lamellarins, but also, getting structurally diversified congeners, which finally embark scientist to shape an integrated and systematic SARs mapping and provide more chemical entities for clinical trials. For recent and detailed advances on their chemical syntheses, see Fukuda et al., .