Total Synthesis of (+)-Cortistatin A: Steroidal Approaches

Abstract

Recent advances in synthetic studies on steroidal alkaloid, (+)-cortistatin A, are described. (+)-Cortistatin A shows a potent and selective anti-angiogenetic activity against human umbilical vein endothelial cells (HUVECs) at nM concentrations and expected as a novel anticancer drug candidate. (+)-Cortistatin A has attracted considerable attention of not only biologists but also synthetic chemists because of its unique highly functionalized abeo-9(10,19)-androstane structure and potent biological activity. Thus the total syntheses of (+)-cortistatin A have been reported by three groups and the synthetic studies are currently underway by several groups. This review focuses on synthetic approaches taking advantage of using steroidal derivatives through ring expansion reaction to construct the core structure of (+)-cortistatin A reported by Corey and Baran respectively.