title: A unified lead-oriented synthesis of over fifty molecular scaffolds.
abstract: Controlling the properties of lead molecules is critical in drug discovery, but sourcing large numbers of lead-like compounds for screening collections is a major challenge. A unified synthetic approach is described that enabled the synthesis of 52 diverse lead-like molecular scaffolds from a minimal set of 13 precursors. The divergent approach exploited a suite of robust, functional group-tolerant transformations. Crucially, after derivatisation, these scaffolds would target significant lead-like chemical space, and complement commercially-available compounds.
authors.affiliation: School of Chemistry, University of Leeds, Leeds, LS2 9JT, UK. s.p.marsden@leeds.ac.uk a.s.nelson@leeds.ac.uk.
authors.forename: Richard G
authors.initials: RG
authors.lastname: Doveston
authors.forename: Paolo
authors.initials: P
authors.lastname: Tosatti
authors.forename: Mark
authors.initials: M
authors.lastname: Dow
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Foley
authors.forename: Ho Yin
authors.initials: HY
authors.lastname: Li
authors.forename: Amanda J
authors.initials: AJ
authors.lastname: Campbell
authors.forename: David
authors.initials: D
authors.lastname: House
authors.forename: Ian
authors.initials: I
authors.lastname: Churcher
authors.forename: Stephen P
authors.initials: SP
authors.lastname: Marsden
authors.forename: Adam
authors.initials: A
authors.lastname: Nelson
mesh_terms: D000588:Amines / Q000737:chemistry*; D002254:Carbonates / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D003500:Cyclization; D015195:Drug Design; D055808:Drug Discovery; D057166:High-Throughput Screening Assays; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000138:chemical synthesis*
chemical_list: D000588:Amines; D002254:Carbonates; D054852:Small Molecule Libraries