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Showing 1–7 of 7 results
Advanced filters: Author: Slava Ziegler Clear advanced filters

  • Natural product–inspired compounds are primed to interact with and manipulate biological processes, but obtaining these complex molecules poses synthetic challenges. The development of a 12-step, 1-pot cascade reaction leads to the 'centrocountins', tetrahydroindoloquinolizines that modulate mitosis by targeting the centrosome-associated proteins nucleophosmin and Crm1.

    • Heiko Dückert
    • Verena Pries
    • Herbert Waldmann
    Research
    Nature Chemical Biology
    Volume: 8, P: 179-184

  • Design strategies that possess both biological relevance and structural diversity may lead to compound collections that are enriched in diverse bioactivities. Now a diverse pseudo-natural product design principle has been established to efficiently explore biologically relevant chemical space. Through dearomatization reactions, a compound collection enriched in both structural and biological diversity was rapidly generated.

    • Sukdev Bag
    • Jie Liu
    • Herbert Waldmann
    ResearchOpen Access
    Nature Chemistry
    Volume: 16, P: 945-958

  • Generating diverse structures with a minimum amount of synthetic effort is an important goal for drug discovery. Here, the authors report a two-phase synthesis for the generation of skeletally diverse small molecules—forming molecular scaffolds and subsequently diversifying each into multiple structures.

    • Miguel Garcia-Castro
    • Lea Kremer
    • Kamal Kumar
    Research
    Nature Communications
    Volume: 6, P: 1-13

  • New natural-product-inspired molecules are often limited by their only partial coverage of biologically relevant chemical space. Combining fragments of natural products has now been shown to yield pseudo natural products, which — while still being inspired by natural products — populate previously unexplored areas of chemical space and have novel biological activities.

    • George Karageorgis
    • Elena S. Reckzeh
    • Herbert Waldmann
    Research
    Nature Chemistry
    Volume: 10, P: 1103-1111

  • The cholesterol-transfer protein GRAMD1A is identified as the target of the autophagy inhibitors autogramin-1 and autogramin-2. GRAMD1A is found to be required for autophagosome biogenesis.

    • Luca Laraia
    • Alexandra Friese
    • Herbert Waldmann
    Research
    Nature Chemical Biology
    Volume: 15, P: 710-720

  • Synthetic methods that efficiently construct structurally diverse molecular scaffolds are attractive routes to diversely bioactive molecules. Here the authors report a method whereby common starting materials are converted to structurally and functionally diverse products by changing the catalyst ligand.

    • Yen-Chun Lee
    • Sumersing Patil
    • Herbert Waldmann
    ResearchOpen Access
    Nature Communications
    Volume: 8, P: 1-12

  • A Lewis-acid-catalysed 1,3-dipolar cycloaddition provides rapid access to a variety of substituted spirooxindoles. Initial cellular evaluations supports the view that compound collections based on natural-product-inspired scaffolds constructed with complex stereochemistry, and decorated with assorted substituents, will be a rich source of compounds with diverse bioactivity.

    • Andrey P. Antonchick
    • Claas Gerding-Reimers
    • Herbert Waldmann
    Research
    Nature Chemistry
    Volume: 2, P: 735-740