ReviewFrontiers in chemistry2018
Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections.
Review in Frontiers in chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed.
- Anomeric Amide Enabled Divergent Synthesis of Unsymmetrical Ureas, Carbamates, Thioesters, and Amides From Aldehydes.Angewandte Chemie (International ed. in English) · 2026Article
- Leveraging fragment-based drug discovery to advance 3D scaffolds into potent ligands: application to the histamine HRSC medicinal chemistry · 2026Article
- New Insights into the French Paradox: Free Radical Scavenging by Resveratrol Yields Cardiovascular Protective Metabolites.Journal of medicinal chemistry · 2025Article
- Exploring Simple Drug Scaffolds from the Generated Database Chemical Space Reveals a Chiral Bicyclic Azepane with Potent Neuropharmacology.Journal of medicinal chemistry · 2025Article
- Unifying principles for the design and evaluation of natural product-inspired compound collections.Chemical science · 2025Review
- 1,3-Dipolar cycloaddition reactions of isatin-derived azomethine ylides for the synthesis of spirooxindole and indole-derived scaffolds: recent developments.Molecular diversity · 2023Review
- Designing of disruptor molecules to restrain the protein-protein interaction network of VANG1/SCRIB/NOS1AP using fragment-based drug discovery techniques.Molecular diversity · 2023Article
- Mining the Protein Data Bank to inspire fragment library design.Frontiers in chemistry · 2023Article
- Exploration of piperidine 3D fragment chemical space: synthesis and 3D shape analysis of fragments derived from 20 regio- and diastereoisomers of methyl substituted pipecolinates.RSC medicinal chemistry · 2022Article
- Diversity-Oriented Synthesis: Amino Acetophenones as Building Blocks for the Synthesis of Natural Product Analogs.Pharmaceuticals (Basel, Switzerland) · 2021Review
- 1,2,3-Triazoles as Biomimetics in Peptide Science.Molecules (Basel, Switzerland) · 2021Review
- Emergent synthetic methods for the modular advancement of spChemical science · 2021Review
- Schistosomiasis Drug Discovery in the Era of Automation and Artificial Intelligence.Frontiers in immunology · 2021Review
- Re-engineering natural products to engage new biological targets.Natural product reports · 2020Article
- AAPH or Peroxynitrite-Induced Biorelevant Oxidation of Methyl Caffeate Yields a Potent Antitumor Metabolite.Biomolecules · 2020Article
- Design and Synthesis of 56 Shape-Diverse 3D Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Diversity Oriented Clicking (DOC): Divergent Synthesis of SuFExable Pharmacophores from 2-Substituted-Alkynyl-1-Sulfonyl Fluoride (SASF) Hubs.Angewandte Chemie (International ed. in English) · 2020Article
- Evaluation of 3-Dimensionality in Approved and Experimental Drug Space.ACS medicinal chemistry letters · 2020Article
- Application of Fragment-Based Drug Discovery to Versatile Targets.Frontiers in molecular biosciences · 2020Review
- Expanding medicinal chemistry into 3D space: metallofragments as 3D scaffolds for fragment-based drug discovery.Chemical science · 2019Article
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Fragment-based drug discovery (FBDD) is a well-established approach for the discovery of novel medicines, illustrated by the approval of two FBBD-derived drugs. This methodology is based on the utilization of small "fragment" molecules (<300 Da) as starting points for drug discovery and optimization. Organic synthesis has been identified as a significant obstacle in FBDD, however, in particular owing to the lack of novel 3-dimensional (3D) fragment collections that feature useful synthetic vectors for modification of hit compounds. Diversity-oriented synthesis (DOS) is a synthetic strategy that aims to efficiently produce compound collections with high levels of structural diversity and three-dimensionality and is therefore well-suited for the construction of novel fragment collections. This Mini-Review highlights recent studies at the intersection of DOS and FBDD aiming to produce novel libraries of diverse, polycyclic, fragment-like compounds, and their application in fragment-based screening projects.
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