Agelastatin A, an alkaloid originally isolated from the marine sponge Agelas dendromorpha, has long been an attractive target of chemical synthesis due to its significant biological activity and unique chemical structure. The synthetic approaches to the agelastatin alkaloid have demonstrated the advances of new methodologies and strategies for accessing a highly functionalized polycyclic nitrogen heterocycle. The present article reviews synthetic endeavors on agelastatin A that have been made by various synthetic chemists as well as biological studies on the natural product and its analogues aimed at the development of medicinal resources.