ArticleChemical science2020
Macrocycle synthesis strategy based on step-wise "adding and reacting" three components enables screening of large combinatorial libraries.
Article in Chemical science, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Accelerate Your Science: Direct-to-Biology Strategies in Medicinal Chemistry.Journal of medicinal chemistry · 2026Review
- Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows.bioRxiv : the preprint server for biology · 2023Article
- Identification of specific carbonic anhydrase inhibitorsRSC medicinal chemistry · 2023Article
- Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale.Nature communications · 2022Article
- Divergent, C-C Bond Forming Macrocyclizations Using Modular Sulfonylhydrazone and Derived Substrates.The Journal of organic chemistry · 2021Article
- Conformational interplay in hybrid peptide-helical aromatic foldamer macrocycles.Chemical science · 2021Article
- Strategies to expand peptide functionality through hybridisation with a small molecule component.RSC chemical biology · 2021Review
Corrections and comments
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Authors and funding
11 authors.
Funding
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Abstract
Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three building blocks are coupled sequentially in efficient alkylation reactions that eliminate the need for product purification. We demonstrate the power of the approach by combinatorially reacting 15 bromoacetamide-activated tripeptides, 42 amines, and 6 bis-electrophile cyclization linkers to generate a 3780-compound library with minimal effort. Screening against thrombin yielded a potent and selective inhibitor (
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