Our Research activity rests its foundation on Complexity-Inspired Organic Synthesis, particularly concerning Target-Oriented Total Synthesis of natural products. Total synthesis of complex molecular architectures has long been recognized as the most powerful form for training synthetic organic chemists and advancing chemical sciences. This historical discipline has a rich and glorious tradition in both teaching and research, and is an indispensible component in any scientific institutions. In addition to the synthetic challenges associated with the unprecedented molecular architectures, total synthesis serves as a platform for uncovering novel chemical reactivities and enables the understanding of chemo-, regio- and stereoselectivities in complex molecular systems. As such, this powerful vehicle for the invention of new synthetic strategies and methodologies, particularly concerning atom-atom bond forming/breaking reactions, catalysis, and asymmetric inductions, has a cemented position in synthetic organic chemistry. In conjunction with the biological properties exhibited by these novel molecular entities, application of synthetic organic chemistry to unfold the mechanism of biological action and the possibility of discovering novel chemotherapeutics is also paramount to the biomedical community.