Synthetic Efforts Towards the Total Synthesis of Erythrina Alkaloids as Potential Therapeutic Agents

Erythrina alkaloids are novel alkaloids isolated from tropical terrestrial flowering plants of the Fabaceae family. Used in folk medicine for centuries, Erythrina alkaloids exhibit antibiotic, anti-malarial, and sedative properties in addition to anticancer effects. These alkaloids offer a broad range of compounds with potential to become therapeutic agents for the treatment of pediatric diseases, particularly central nervous system malignancies. The important biological properties of these alkaloids fueled our continuous effort to find new drug leads, and we have developed an efficient synthetic route to the erythrin core using novel alkylation reactions. Compounds were purified and characterized utilizing column chromatography, UPLC-MS, and NMR techniques.

Using new synthetic methodologies, we have developed a feasible route to obtain the erythrin core in multigram quantities for the development of a library in an enantioselective manner. In collaboration with our departmental screening facility, we will screen our analogs against St. Jude’s collection of solid tumor and hematology cancer cell line panels as well as malaria and antibiotic resistant strains.