Total Synthesis as a Resource in the Discovery of Potentially Valuable Antitumor Agents: Cycloproparadicicol

Abstract

A highly convergent synthesis was used to prepare a series of epimers and analogues of radicicol (1). Biological assessment revealed a previously unrecognized correlation between stereochemistry and antitumor potential in these compounds. Significantly, cycloproparadicicol (2) showed promising therapeutic properties based on inhibition of chaperones.