ArticleChemical science2015
Macrocycles: lessons from the distant past, recent developments, and future directions.
Article in Chemical science, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 132 papers.
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Who cites it
132 citing papers in PubMed, 481 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
- MEGPNM as a multiscale edge-aware GAT network with hybrid pooling predicting permeability of non-peptidic macrocycles.Communications chemistry · 2026Article
- Successive Ring Expansion Strategies for the Synthesis of Macrocycles and Medium-Sized Rings.Chemical reviews · 2026Article
- Non-Dilute Synthesis of Macrodiolides and Macrotetrolides Enabled by Confinement Catalysis.Angewandte Chemie (International ed. in English) · 2026Article
- Synthesis of Macrocyclic Structures by Intramolecular Photoclick Reaction.Journal of the American Chemical Society · 2026Article
- Modular Assembly of Macrocyclic Sulfonamides via Consecutive Cascade Ring Expansion Reactions.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Natural Products Beyond Inhibition: A Mechanistic Framework Spanning Pockets, Interfaces, and Kinetic Barriers.Molecules (Basel, Switzerland) · 2026Review
- A novel entry inhibitor targeting the stalk domain of the hemagglutinin of H1N1.Acta pharmaceutica Sinica. B · 2026Article
- Synthesis of the Proposed Structure of Celacarfurine and Analogues Using Sequential Cascade Ring Expansion Reactions.Organic letters · 2026Article
- Modular Synthesis of Pyritide-Inspired Macrocycles Featuring Bipyridine Motifs.Angewandte Chemie (International ed. in English) · 2025Article
- Chemoselective sulfonyl fluoride exchange (SuFEx)-induced macrocyclization of tyrosine-containing peptides in aqueous media.Chemical science · 2025Article
- Macrocyclic Peptides Containing an Imidazopyridinium (IPbioRxiv : the preprint server for biology · 2025Article
- Encapsulation of an Electron in a Diborencine Macrocycle: Synthesis, Structure, and Reactivity.Journal of the American Chemical Society · 2025Article
- Article
- Stereocontrolled four-carbon homologation of vicinally functionalized allylic pyrrolidines to highly customized azonines bearing remote benzylic stereocenters.RSC advances · 2025Article
- Application of Free Energy Perturbation (FEP) Methodology for Predicting the Binding Affinity of Macrocyclic JAK2 Inhibitor Analogues of Pacritinib.ACS medicinal chemistry letters · 2025Article
- Antimicrobial Peptide-Peptoid Macrocycles from the Polymyxin B2 Chemical Space.Angewandte Chemie (International ed. in English) · 2025Article
- Expanding Automated Multiconformer Ligand Modeling to Macrocycles and Fragments.bioRxiv : the preprint server for biology · 2025Article
- End-to-End Backbone Cyclization Enhances Passive Permeability of bRo5 Oligomeric Depsipeptides with Nonlinear Size Dependence.ACS medicinal chemistry letters · 2025Article
- Unifying principles for the design and evaluation of natural product-inspired compound collections.Chemical science · 2025Review
72 more citing papers are in PubMed but not listed here.
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Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A noticeable increase in molecular complexity of drug targets has created an unmet need in the therapeutic agents that are larger than traditional small molecules. Macrocycles, which are cyclic compounds comprising 12 atoms or more, are now recognized as molecules that "are up to the task" to interrogate extended protein interfaces. However, because macrocycles (particularly the ones based on peptides) are equipped with large polar surface areas, achieving cellular permeability and bioavailability is anything but straightforward. While one might consider this to be the Achilles' heel of this class of compounds, the synthetic community continues to develop creative approaches toward the synthesis of macrocycles and their site-selective modification. This perspective provides an overview of both mechanistic and structural issues that bear on macrocycles as a unique class of molecules. The reader is offered a historical foray into some of the classic studies that have resulted in the current renaissance of macrocycles. In addition, an attempt is made to overview the more recent developments that give hope that macrocycles might indeed turn into a useful therapeutic modality.
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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.