ArticleACS medicinal chemistry letters2016
Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
What it found
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Who cites it
12 citing papers in PubMed.
- Natural Product-like Fragments Unlock Novel Chemotypes for a Kinase Target─Exploring Options beyond the Flatland.Journal of chemical information and modeling · 2026Article
- New Insights into the French Paradox: Free Radical Scavenging by Resveratrol Yields Cardiovascular Protective Metabolites.Journal of medicinal chemistry · 2025Article
- Chemoenzymatic Asymmetric Synthesis of Complex Heterocycles: Dihydrobenzoxazinones and Dihydroquinoxalinones.ACS catalysis · 2022Article
- Supported Gold Nanoparticle-Catalyzed Selective Reduction of Multifunctional, Aromatic Nitro Precursors into Amines and Synthesis of 3,4-Dihydroquinoxalin-2-Ones.Molecules (Basel, Switzerland) · 2022Article
- N-terminal phosphorylation regulates the activity of glycogen synthase kinase 3 from Plasmodium falciparum.The Biochemical journal · 2022Article
- Design and Synthesis of 56 Shape-Diverse 3D Fragments.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.Chemical science · 2020Article
- Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains.ACS medicinal chemistry letters · 2019Article
- Samarium(II) folding cascades involving hydrogen atom transfer for the synthesis of complex polycycles.Nature communications · 2018Article
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections.Frontiers in chemistry · 2018Review
- Synthesis and Demonstration of the Biological Relevance of spChemistry (Weinheim an der Bergstrasse, Germany) · 2017Article
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
Traditional fragment-based drug discovery (FBDD) relies heavily on structural analysis of the hits bound to their targets. Herein, we present a complementary approach based on diversity-oriented synthesis (DOS). A DOS-based fragment collection was able to produce initial hit compounds against the target GSK3β, allow the systematic synthesis of related fragment analogues to explore fragment-level structure-activity relationship, and finally lead to the synthesis of a more potent compound.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.