Diversity-Oriented Synthesis as a Tool for Chemical Genetics

Molecules

Elena Lenci¹  Antonio Guarna¹ 

[1] id="af1-molecules-19-16506">Department of Chemistry “Ugo Schiff”, University of Florence, via della Lastruccia 13, I-50019 Sesto Fiorentino, Florence, Ita

关键词: diversity-oriented synthesis;    chemical genetics;    drug discovery;    chemical biology;    small molecules;    high-throughput screening;   

DOI  :  10.3390/molecules191016506

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.