Diversity Oriented Synthesis: A Challenge for Synthetic Chemists.

Autor: Stock, G., Lessl, M., Jaroch, S., Weinmann, H., Bender, A., Fergus, S., Galloway, W. R. J. D., Glansdorp, F. G., Marsden, D. M., Nicholson, R. L., Spandl, R. J., Thomas, G. L., Wyatt, E. E., Glen, R. C., Spring, D. R.
Zdroj: Chemical Genomics; 2006, p47-60, 14p
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 disadvantageswith 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. [ABSTRACT FROM AUTHOR]
Databáze: Supplemental Index