Solid-phase synthesis of a pepticinnamin E library.

Pepticinnamin E is a naturally occurring bisubstrate inhibitor of farnesyltransferase. Based on the structure of the natural product, a compound library was synthesized by variation of eight structural parameters. Following three different routes, a total of 51 analogues was synthesized on the polymeric support in 6-11-step parallel syntheses. Overall yields ranged from 3 to 63%, and the compounds were obtained with >90% purity.