ArticleProceedings of the National Academy of Sciences of the United States of America2011
Diversity-oriented synthesis of macrocyclic peptidomimetics.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 115 citations in OpenAlex.
- Beyond Simple Mimicry: Next-Generation Geometric Architectures and Future Paradigms in Small-Molecule and Macrocyclic Peptidomimetics.Angewandte Chemie (International ed. in English) · 2026Review
- Modular Assembly of Macrocyclic Sulfonamides via Consecutive Cascade Ring Expansion Reactions.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Enantio-, atrop-, and diastereoselective macrolactonization to access type III cyclophanes.Nature communications · 2025Article
- Recent Progress on Synthesis of Functionalized 1,5-Disubstituted Triazoles.Current organic synthesis · 2024Review
- DLiP-PPI library: An integrated chemical database of small-to-medium-sized molecules targeting protein-protein interactions.Frontiers in chemistry · 2022Article
- Coupling Interrupted Fischer and Multicomponent Joullié-Ugi to Chase Chemical Diversity: from Batch to Sustainable Flow Synthesis of Peptidomimetics.ChemMedChem · 2021Article
- iVS analysis to evaluate the impact of scaffold diversity in the binding to cellular targets relevant in cancer.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands.Science advances · 2019Article
- Multidirectional desymmetrization of pluripotent building block en route to diastereoselective synthesis of complex nature-inspired scaffolds.Nature communications · 2018Article
- Synthesis of novel cyclopeptides containing heterocyclic skeletons.RSC advances · 2018Review
- Recent Applications of Diversity-Oriented Synthesis Toward Novel, 3-Dimensional Fragment Collections.Frontiers in chemistry · 2018Review
- Computer-aided design of amino acid-based therapeutics: a review.Drug design, development and therapy · 2018Review
- Direct Substitution of Arylalkynyl Carbinols Provides Access to Diverse Terminal Acetylene Building Blocks.Organic letters · 2017Article
- An eco-compatible strategy for the diversity-oriented synthesis of macrocycles exploiting carbohydrate-derived building blocks.Beilstein journal of organic chemistry · 2017Article
- A Multidimensional Diversity-Oriented Synthesis Strategy for Structurally Diverse and Complex Macrocycles.Angewandte Chemie (International ed. in English) · 2016Article
- Cheminformatics Research at the Unilever Centre for Molecular Science Informatics Cambridge.Molecular informatics · 2015Article
- A diversity-oriented synthesis strategy enabling the combinatorial-type variation of macrocyclic peptidomimetic scaffolds.Organic & biomolecular chemistry · 2015Article
- Large ring-forming alkylations provide facile access to composite macrocycles.Chemical science · 2015Article
- Strategy to discover diverse optimal molecules in the small molecule universe.Journal of chemical information and modeling · 2015Article
- Conformational properties of 1,4- and 1,5-substituted 1,2,3-triazole amino acids – building units for peptidic foldamers.Organic & biomolecular chemistry · 2015Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Structurally diverse libraries of novel small molecules represent important sources of biologically active agents. In this paper we report the development of a diversity-oriented synthesis strategy for the generation of diverse small molecules based around a common macrocyclic peptidomimetic framework, containing structural motifs present in many naturally occurring bioactive compounds. Macrocyclic peptidomimetics are largely underrepresented in current small-molecule screening collections owing primarily to synthetic intractability; thus novel molecules based around these structures represent targets of significant interest, both from a biological and a synthetic perspective. In a proof-of-concept study, the synthesis of a library of 14 such compounds was achieved. Analysis of chemical space coverage confirmed that the compound structures indeed occupy underrepresented areas of chemistry in screening collections. Crucial to the success of this approach was the development of novel methodologies for the macrocyclic ring closure of chiral α-azido acids and for the synthesis of diketopiperazines using solid-supported N methylmorpholine. Owing to their robust and flexible natures, it is envisaged that both new methodologies will prove to be valuable in a wider synthetic context.
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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.