Total synthesis, chemical modification and structure-activity relationship of bufadienolides

Abstract Bufadienolides are a type of natural cardiac steroids and originally isolated from the Traditional Chinese Medicine Chan’Su, they have been used for the treatment of heart disease in traditional remedies as well as in modern medicinal therapy with potent anti-tumor activities. Due to their unique molecular structures with unsaturated six-membered lactones attached to the steroid core, bufadienolides have received great attention in the synthetic organic community. This review presents total synthetic efforts to some representative bufadienolides, chemical modification of bufadienolides will also be given to discuss their structure-activity relationship in anti-tumor.