Solid-phase synthesis in lead optimization and drug discovery.

Solid-phase synthesis is a valuable tool for drug discovery research. The value is particularly evident in lead optimization work where it contributes to the rapid and thorough identification of the optimal drug candidate within a lead series. Solid-phase synthesis methods continue to be developed at a rapid pace, and these methods will eventually become standard tools for medicinal chemists. This review is focused on papers published since the beginning of 1998, which describe the use of solid-phase synthesis in lead optimization.