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Issue 4, 2008
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Natural products as an inspiration in the diversity-oriented synthesis of bioactive compound libraries

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Abstract

Covering: up to the end of August 2007

The purpose of diversity-oriented synthesis is to drive the discovery of small molecules with previously unknown biological functions. Natural products necessarily populate biologically relevant chemical space, since they bind both their biosynthetic enzymes and their target macromolecules. Natural product families are, therefore, libraries of pre-validated, functionally diverse structures in which individual compounds selectively modulate unrelated macromolecular targets. This review describes examples of diversity-oriented syntheses which have, to some extent, been inspired by the structures of natural products. Particular emphasis is placed on innovations that allow the synthesis of compound libraries that, like natural products, are skeletally diverse. Mimicking the broad structural features of natural products may allow the discovery of compounds that modulate the functions of macromolecules for which ligands are not known. The ability of innovations in diversity-oriented synthesis to deliver such compounds is critically assessed.

Graphical abstract: Natural products as an inspiration in the diversity-oriented synthesis of bioactive compound libraries

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Publication details

The article was received on 18 Feb 2008 and first published on 14 Apr 2008


Article type: Review Article
DOI: 10.1039/B706296F
Nat. Prod. Rep., 2008,25, 719-737
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    Natural products as an inspiration in the diversity-oriented synthesis of bioactive compound libraries

    C. Cordier, D. Morton, S. Murrison, A. Nelson and C. O'Leary-Steele, Nat. Prod. Rep., 2008, 25, 719
    DOI: 10.1039/B706296F

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