Current strategies for diversity-oriented synthesis

Compounds accessed through diversity-oriented synthesis (DOS) are showing promise in modulating the activities of several targets that are currently considered ‘undruggable’. Recently many new DOS pathways have been developed employing multi-component reactions, cycloadditions, ring-closing metathesis and tandem processes. Functional group pairing and ‘build/couple/pair’ strategies have been described as a means for generating structural diversity. Efforts have also been directed towards developing DOS libraries based on privileged scaffolds. Recent studies have provided several compelling examples for the utility of DOS compounds for producing novel biological probes and application of DOS in the context of drug discovery is extremely appealing.