Diversity-Oriented Synthesis: Developing New Chemical Tools to Probe and Modulate Biological Systems

Warren R. J. D. Galloway, David Wilcke, Feilin Nie, Kathy Hadje-Georgiou, Luca Laraia, David R. Spring

Research output: Chapter in Book/Report/Conference proceedingBook chapterResearchpeer-review


Biologically active small molecules can be identified through the screening of compound libraries. Traditionally, such libraries were composed of large numbers of structurally similar compounds. However, it is now widely acknowledged that library size is not everything; the structural diversity of the library is crucial. Structurally diverse small molecule libraries should contain compounds with a broad range of biological activities, which are capable of providing compounds active against a variety of biological targets. Diversity-oriented synthesis (DOS) seeks to generate structurally diverse small-molecule libraries in an efficient manner. Here, we discuss the general principles of DOS. A case study describing the discovery of new small-molecule modulators of mitosis using DOS illustrates the utility of this approach in the identification of new biologically relevant chemical entities.
Original languageEnglish
Title of host publicationConcepts and Case Studies in Chemical Biology
EditorsH. Waldmann, P. Janning
Publication date2014
ISBN (Print)9783527336111
ISBN (Electronic)9783527687503
Publication statusPublished - 2014
Externally publishedYes
SeriesConcepts and Case Studies in Chemical Biology


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