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Molecules 2014, 19(10), 16506-16528; doi:10.3390/molecules191016506

Diversity-Oriented Synthesis as a Tool for Chemical Genetics

Department of Chemistry "Ugo Schiff", University of Florence, via della Lastruccia 13, I-50019 Sesto Fiorentino, Florence, Italy
Author to whom correspondence should be addressed.
Received: 22 August 2014 / Revised: 30 September 2014 / Accepted: 1 October 2014 / Published: 14 October 2014
(This article belongs to the Special Issue Recent Advances in Diversity-Oriented Synthesis)
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Chemical genetics is an approach for identifying small molecules with the ability to induce a biological phenotype or to interact with a particular gene product, and it is an emerging tool for lead generation in drug discovery. Accordingly, there is a need for efficient and versatile synthetic processes capable of generating complex and diverse molecular libraries, and Diversity-Oriented Synthesis (DOS) of small molecules is the concept of choice to give access to new chemotypes with high chemical diversity. In this review, the combination of chemical genetics and diversity-oriented synthesis to identify new chemotypes as hit compounds in chemical biology and drug discovery is reported, giving an overview of basic concepts and selected case studies. View Full-Text
Keywords: diversity-oriented synthesis; chemical genetics; drug discovery; chemical biology; small molecules; high-throughput screening diversity-oriented synthesis; chemical genetics; drug discovery; chemical biology; small molecules; high-throughput screening

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Lenci, E.; Guarna, A.; Trabocchi, A. Diversity-Oriented Synthesis as a Tool for Chemical Genetics. Molecules 2014, 19, 16506-16528.

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