title: Scaffold Diversity Synthesis and Its Application in Probe and Drug Discovery.
abstract: Scaffold diversity is a crucial feature of compound collections that has a huge impact on their success in biological screenings. The synthesis of highly complex and diverse scaffolds, which could be based on natural products, for example, is an arduous task that requires expertise in various aspects of organic synthesis and structural analysis. This challenge has been addressed by a number of synthesis designs, which employ natural products as a source of scaffold diversity, transform suitably designed common intermediates into various molecular frameworks, or entail highly concise synthetic routes to a number of distinct and complex scaffolds. In this Minireview, we highlight recent synthetic developments towards the construction of diverse and complex scaffolds and the application of the resulting compound collections in drug and probe discovery.
authors.affiliation: Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
authors.forename: Miguel
authors.initials: M
authors.lastname: Garcia-Castro
authors.affiliation: Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Zimmermann
authors.affiliation: Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany.
authors.forename: Muthukumar G
authors.initials: MG
authors.lastname: Sankar
authors.affiliation: Department of Chemical Biology, Max Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227, Dortmund, Germany. kamal.kumar@mpi-dortmund.mpg.de.
authors.forename: Kamal
authors.initials: K
authors.lastname: Kumar
mesh_terms: D000469:Alkaline Phosphatase / Q000737:chemistry / Q000378:metabolism; D000470:Alkaloids / Q000138:chemical synthesis / Q000737:chemistry; D001688:Biological Products / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D055808:Drug Discovery; D006801:Humans; D056004:Molecular Dynamics Simulation; D045788:Sesquiterpenes, Germacrane / Q000138:chemical synthesis / Q000737:chemistry; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000470:Alkaloids; D001688:Biological Products; D045788:Sesquiterpenes, Germacrane; D054852:Small Molecule Libraries; D000469:Alkaline Phosphatase
keywords: compound collections; drug discovery; natural products; scaffold diversity; scaffold synthesis