Flavaglines: Their Discovery from Plants Used in Traditional Chinese Medicine, Synthesis, and Drug Development Against Cancer and Immune Disorders

Abstract

: Flavaglines, a family of compounds coming from plants used in Traditional Chinese Medicine, exhibit a broad range of biological effects including anticancer, antiviral, cardioprotectant and anti-inflammatory activities. They exert their action by targeting the scaffold proteins called prohitins-1 and-2, and the mRNA helicases eIF4A and DDX3. Flavaglines are densely functionalized cyclopenta[b]benzofurans that have attracted the attention of some of the most eminent organic chemists. This review provides an overview of the biosynthesis, total synthesis and pharmacological activities of flavaglines, which recently culminated with the entrance of a synthetic derivative, Zotatifin, into clinical trials against advanced solid tumors refractory or intolerant to standard treatments.