Executive Summary : | Guaianolide sesquiterpene lactones (GSLs) are a major class of plant secondary metabolites with hundreds of members and new ones continuously added. These guaianolides have a 5, 7, 5-ring system and exhibit a broad spectrum of biological activities, including antitumor, anti-inflammatory, anti-Alzheimer's, and antimicrobial properties. Their alluring potential in therapeutics and challenging chemical structures have generated significant traction among the medicinal and synthetic chemistry community. To discover more promising pharmaceutical lead compounds from GSLs, new and unified synthetic routes are needed. A research proposal is being proposed to target the total synthesis and Diversity Oriented Synthesis (DOS) of guaiane-based natural products with implications in diseases like Alzheimer's disease, cancer, and inflammation. A flexible and multipronged approach is needed to explore the vast chemical diversity around these molecular architects. The synthetic route is expected to be multidimensional, targeting several members from this family through a unified approach. Subtle variations in the synthetic strategy at various stages of execution will also aid in developing diversity-oriented synthetic routes. |