Natural products are the most rewarding source of new chemotherapeutics. It is estimated that nearly half of small organic molecules approved by FDA for treatment of cancers are natural products or their analogues/derivatives. In the field of infectious diseases, discovery of structurally novel antibacterial natural products is decisive to the development of new antimicrobial agents. However, natural products are isolated from natural sources in small quantities. This becomes the main obstacle that prevents many bioactive natural products from being developed into clinically used medicines.
Chemical synthesis is highly desirable to supply sufficient material for various bioassays, and more importantly allows access to a collection of structural analogs that may reveal the key pharmacophore. Chemical synthesis of natural products may provide many additional benefits, such as confirmation of molecular structures and inspiration of new synthetic methodologies.
Our short and reliable synthetic route provides a supply of anthracimycins for further in-depth studies and allows medicinal chemists to prepare a library of analogues for establishing structure-activity relationship.