title: Design and Synthesis of Fsp(3)-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening.
abstract: The exploration of innovative chemical space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biologically relevant metabolites and show attractive features, such as molecular compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available commercial reagents and robust chemical transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented.
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Silvia
authors.initials: S
authors.lastname: Stotani
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Christoph
authors.initials: C
authors.lastname: Lorenz
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Matthias
authors.initials: M
authors.lastname: Winkler
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Federico
authors.initials: F
authors.lastname: Medda
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Edwige
authors.initials: E
authors.lastname: Picazo
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Raquel
authors.initials: R
authors.lastname: Ortega Martinez
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Anna
authors.initials: A
authors.lastname: Karawajczyk
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Jorge
authors.initials: J
authors.lastname: Sanchez-Quesada
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG , Emil-Figge-Strasse 76a, 44227 Dortmund, Germany.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Giordanetto
mesh_terms: D061565:Cycloaddition Reaction; D015195:Drug Design; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D057166:High-Throughput Screening Assays; D007202:Indicators and Reagents; D008958:Models, Molecular; D008968:Molecular Conformation; D054852:Small Molecule Libraries; D013237:Stereoisomerism
chemical_list: D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D054852:Small Molecule Libraries
keywords: European Lead Factory; compound library design; compound library synthesis; spirocenter; spirocyclic