Solution-phase synthesis in combinatorial chemistry: Applications in drug discovery

Abstract

The application of combinatorial chemistry principles to produce libraries of compounds, together with effective use of high-throughput biological screening, is set to revolutionize the way in which chemical leads for drug discovery programmes are generated and evaluated. In this overview, solution-phase synthesis is compared and contrasted with solid-phase synthesis, which remains the method of choice for most combinatorial library work. The author discusses a variety of specific approaches from different groups exemplifying the potential of solution-phase work.