An alarming increase in cancer deaths around the globe has sparked a quest for new effective antitumor drugs developed through biological screening of both terrestrial and marine organisms. Recently, analyses of marine-derived alkaloids isolated from tunicates, a close relative to vertebrates, reveal various anti-cancer activities including anti-angiogenic action, anti-proliferative activity, inhibition of key cellular events like topoisomerase function and tubulin polymerization with respect to cytotoxicity and apoptosis. Vast numbers of potential anticancer molecules in the marine biosphere cannot be underestimated. Tunicate compounds have already entered the market and shown significant success. Moreover, improved technology has enabled synthesis of these molecules by a diverse cadre of professionals including career biologists, immunobiologists, invertebrate immunologists, and marine biologists who use an amazing array of procedures. Although there are no guarantees of consistently reliable success, identifying and comprehending the basic nature of these compounds is a promising first step towards unique pharmaceutical designs that promise to provide a therapeutic solution.