title: Diversity-oriented synthesis: producing chemical tools for dissecting biology.
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.
authors.affiliation: University of Cambridge, Department of Chemistry, Lensfield Road, Cambridge, United Kingdom CB2 1EW.
authors.forename: Cornelius J
authors.initials: CJ
authors.lastname: O' Connor
authors.forename: Henning S G
authors.initials: HS
authors.lastname: Beckmann
authors.forename: David R
authors.initials: DR
authors.lastname: Spring
mesh_terms: D000818:Animals; D001671:Biochemistry / Q000379:methods*; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D051379:Mice; D008954:Models, Biological; D008958:Models, Molecular; D004364:Pharmaceutical Preparations / Q000737:chemistry; D011506:Proteins / Q000737:chemistry; D054852:Small Molecule Libraries
chemical_list: D004364:Pharmaceutical Preparations; D011506:Proteins; D054852:Small Molecule Libraries