Autor: |
Bender A; Department of Chemistry, University of Cambridge, UK. ab454@cam.ac.uk, Fergus S, Galloway WR, Glansdorp FG, Marsden DM, Nicholson RL, Spandl RJ, Thomas GL, Wyatt EE, Glen RC, Spring DR |
Jazyk: |
angličtina |
Zdroj: |
Ernst Schering Research Foundation workshop [Ernst Schering Res Found Workshop] 2006 (58), pp. 47-60. |
DOI: |
10.1007/978-3-540-37635-4_4 |
Abstrakt: |
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. |
Databáze: |
MEDLINE |
Externí odkaz: |
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