ArticleNature chemistry2025
Enantioselective photocatalytic synthesis of bicyclo[2.1.1]hexanes as ortho-disubstituted benzene bioisosteres with improved biological activity.
Article in Nature chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- On-DNA photochemical methods for expanding DNA-encoded library (DEL) chemical space.RSC medicinal chemistry · 2026Review
- Excitation of acyclic trisubstituted alkenes via triplet energy transfer for diastereo- and enantioselective [2 + 2] photocycloaddition.Nature communications · 2026Article
- Programmable regiodivergent light-driven cyclization of acyclic 1,5-dienes unlocks rigid bicyclic architectures.Nature chemistry · 2026Article
- Catalytic endo-stereoselective [2+2] cycloaddition of norbornadienes with internal alkynes.Nature chemistry · 2026Article
- Concise synthesis and strain-release diversification of bridgehead-substituted [2]-ladderanes.Nature chemistry · 2026Article
- Pd-Catalyzed De Novo Skeletal Editing of Bicyclic Carbamates Delivers 2-Pyrimidinones.Organic letters · 2026Article
- Beyond para- and meta-Substitution: Synthesis and Biological Validation of Chalcogen-Rich Thiabicyclo[3.1.1]heptanes as Bioisosteres of Aryl Thioether Derivatives.Angewandte Chemie (International ed. in English) · 2026Article
- Electrochemical synthesis of 2-oxa-bicyclo[2.1.1]hexanes by anodic oxidation-cyclization relay strategy.Chemical science · 2026Article
- Collective synthesis of 1,2,4-trisubstituted, meta- and ortho-substituted arene bioisosteres from bicyclobutanes.Nature chemistry · 2026Article
- Enantioselective Synthesis of 2-Oxabicyclo[2.1.1]hexanes and Bicyclo[2.1.1]hexanes via Catalytic Asymmetric Intramolecular Photocycloadditions.Nature communications · 2026Article
- Boron-Enabled Stereoselective Synthesis of Polysubstituted Housanes.Journal of the American Chemical Society · 2025Article
- Catalyst-Controlled Divergent Synthesis of Bicyclo[2.1.1]hexanes and Cyclobutenes: The Unique Effect of Au(I).JACS Au · 2025Article
- Three-dimensional saturated C(spNature reviews. Chemistry · 2024Review
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10 authors.
Funding
Abstract
1,5-Disubstituted bicyclo[2.1.1]hexanes are bridged scaffolds with well-defined exit vectors that are becoming increasingly popular building blocks in medicinal chemistry because they are saturated bioisosteres of ortho-substituted phenyl rings. Here we have developed a Lewis-acid-catalysed [2 + 2] photocycloaddition to obtain these motifs as enantioenriched scaffolds, providing an efficient approach for their incorporation in a variety of drug analogues. Retention of the biological activity of the bicyclo[2.1.1]hexane-containing analogues in the specific proteins targeted by the original drugs has confirmed the suitability of this moiety to serve as a bioisostere of ortho-substituted phenyl rings. Moreover, we have studied the potential of the different enantiomers of the drug analogues to selectively induce cytotoxicity in a panel of tumour cell lines, observing markedly differential effects for the two enantiomers and a substantial improvement over the corresponding sp
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