Abstract
This article covers the diversity-oriented synthesis (DOS) of small molecules in order to generate a collection of pure compounds that are attractive for lead generation in a phenotypic, high-throughput screening approach useful for chemical genetics and drug discovery programmes. Nature synthesizes a rich structural diversity of small molecules, however, unfortunately, there are some disadvantages with using natural product sources for diverse small-molecule discovery. Nevertheless we have a lot to learn from nature. The efficient chemical synthesis of structural diversity (and complexity) is the aim of DOS. Highlights of this article include a discussion of nature’s and synthetic chemists’ strategies to obtain structural diversity and an analysis of molecular descriptors used to classify compounds. The assessment of how successful one diversity-oriented synthesis is vs another is subjective; therefore we use freely available software (www.cheminformatics.org/diversity) to assess structural diversity in any combinatorial synthesis.
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© 2006 Springer-Verlag Berlin Heidelberg
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Bender, A. et al. (2006). Diversity Oriented Synthesis: A Challenge for Synthetic Chemists. In: Jaroch, S., Weinmann, H. (eds) Chemical Genomics. Ernst Schering Research Foundation Workshop, vol 58. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-37635-4_4
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DOI: https://doi.org/10.1007/978-3-540-37635-4_4
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