Marine natural products have played an important role in the discovery of novel biologically active compounds. Thyrsiferol was originally isolated off the coast of New Zealand from a marine red algae of the genus Laurencia. Several analogues having similar structural features have been identified and their biological properties investigated and identified. The array of activities is significant and includes: cytotoxic, anti-viral, and anti-tumor activity, the specific inhibition of protein serine/threonine phosphatase 2A, and apoptotic cell death in human leukemic T- and B-cell lines. Therefore, it is of interest to design and develop methods that would make these compounds accessible in the laboratory through synthetic organic chemistry. This review will discuss the biological properties and synthetic endeavors that have been used to access thyrsiferol and related analogues.