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Diversity-oriented synthesis: producing chemical tools for dissecting biology.

Authors :
O' Connor CJ
Beckmann HS
Spring DR
Source :
Chemical Society reviews [Chem Soc Rev] 2012 Jun 21; Vol. 41 (12), pp. 4444-56. Date of Electronic Publication: 2012 Apr 10.
Publication Year :
2012

Abstract

Small molecule modulators of biological function can be discovered by the screening of compound libraries. However, it became apparent that some human disease related targets could not be addressed by the libraries commonly used which typically are comprised of large numbers of structurally similar compounds. The last decade has seen a paradigm shift in library construction, with particular emphasis now being placed on increasing a library's structural, and thus functional diversity, rather than only its size. Diversity-oriented synthesis (DOS) aims to generate such structural diversity efficiently. This tutorial review has been written to introduce the subject to a broad audience and recent achievements in both the preparation and the screening of structurally diverse compound collections against so-called 'undruggable' targets are highlighted.

Details

Language :
English
ISSN :
1460-4744
Volume :
41
Issue :
12
Database :
MEDLINE
Journal :
Chemical Society reviews
Publication Type :
Academic Journal
Accession number :
22491328
Full Text :
https://doi.org/10.1039/c2cs35023h