Novel toxic metabolites from marine cyanobacteria have been thoroughly explored. Biologically active and chemically diverse compounds that could be hepatotoxic, neurotoxic or cytotoxic, such as cyclic peptides, lipopeptides, fatty acid amides, alkaloids and saccharides, have been produced from marine cyanobacteria. Many reports have revealed that biosynthesis of active metabolites is predominant during cyanobacterial bloom formation. Marine cyanobacterial toxic metabolites exhibit important biological properties, such as interfering in signal transduction either by activation or blockage of sodium channels or by targeting signaling proteins; inducing apoptosis by disrupting cytoskeletal proteins; and inhibiting membrane transporters, receptors, serine proteases and topoisomerases. The pharmacological importance of these metabolites resides in their proliferation and growth-controlling abilities towards cancer cell lines and disease-causing potent microbial agents (bacteria, virus, fungi and protozoa). Besides their toxic and pharmacological potentials, the present review discusses structural and functional resemblance of marine cyanobacterial metabolites to marine algae, sponges and mollusks. Copyright © 2011 John Wiley & Sons, Ltd.