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Issue 12, 2012
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Diversity-oriented synthesis: producing chemical tools for dissecting biology

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Abstract

Small molecule modulators of biological function can be discovered by the screening of compound libraries. However, it became apparent that some human disease related targets could not be addressed by the libraries commonly used which typically are comprised of large numbers of structurally similar compounds. The last decade has seen a paradigm shift in library construction, with particular emphasis now being placed on increasing a library's structural, and thus functional diversity, rather than only its size. Diversity-oriented synthesis (DOS) aims to generate such structural diversity efficiently. This tutorial review has been written to introduce the subject to a broad audience and recent achievements in both the preparation and the screening of structurally diverse compound collections against so-called ‘undruggable’ targets are highlighted.

Graphical abstract: Diversity-oriented synthesis: producing chemical tools for dissecting biology

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Publication details

The article was received on 26 Jan 2012 and first published on 10 Apr 2012


Article type: Tutorial Review
DOI: 10.1039/C2CS35023H
Citation: Chem. Soc. Rev., 2012,41, 4444-4456
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    Diversity-oriented synthesis: producing chemical tools for dissecting biology

    C. J. O' Connor, H. S. G. Beckmann and D. R. Spring, Chem. Soc. Rev., 2012, 41, 4444
    DOI: 10.1039/C2CS35023H

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