Dynemicin, Uncialamycin, and anthraquinonic derivatives are natural compounds wtih potent antibacterial and anticancer activities due to their unique enediyne moiety. The purpose of this book is to describe the isolation of Dynemicin and Uncialamycin, to provide a brief overview of their biological activities (and potential development as drugs) and to present the various synthetic routes to prepare these compounds as well as analogues. One of the main strengths of this topic is the coverage of a complete field of organic chemistry at the interface with biological science. This ranges from the isolation to the synthesis of natural products (and analogues) possessing enediyne and anthraquinone moieties via their biological activities. Presents two natural ènediynes with similar structures whose total syntheses have been accomplished, Explores structural analogs of preparation for purposes of optimizing the anti-cancer activity. The total syntheses of dynemicin A, the uncialamycine, as well as analogs are described by emphasizing the synthesis strategies adopted. Featuring studies of the biological activities and data to bring out the structural elements of these essential compounds in these activities.