ABSTRACT

The role of natural products in drug discovery has experienced many changes over the past two decades, from a decline in participation by pharmaceutical companies in the 1990s to a renaissance in recent years. In 2007, Newman and Cragg published a comprehensive review analyzing the sources of new drugs, covering the period from 1981 to the middle of 2006 (Newman and Cragg 2007). This analysis demonstrated that more than 60% of new drugs are natural products or natural product-inspired molecules. The potential for nding important new compounds of diverse skeletons in the marine environment is tremendous. More than 10,000 compounds have already been discovered from the marine environment. Examples of approved drugs developed from marine natural products are Ziconotide (Prialt®), Trabectedin (Yondelis®), and Eribulin (Halaven®). Concomitantly at least 20 marine natural products or derivatives are currently being tested in human trials. In this review, synthesis and biological activity of two promising azole marine products, namely, largazole and neopeltolide, will be taken into account.