ArticleAngewandte Chemie (International ed. in English)2017
Two-Step Synthesis of Complex Artificial Macrocyclic Compounds.
Article in Angewandte Chemie (International ed. in English), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- Multicomponent Macrocyclic IL-17a Modifier.ACS medicinal chemistry letters · 2022Article
- Aza-Oxa-Triazole Based Macrocycles with Tunable Properties: Design, Synthesis, and Bioactivity.Molecules (Basel, Switzerland) · 2022Article
- Benchmark of Generic Shapes for Macrocycles.Journal of chemical information and modeling · 2020Article
- Rapid approach to complex boronic acids.Science advances · 2019Article
- A fluorinated indole-based MDM2 antagonist selectively inhibits the growth of p53The FEBS journal · 2019Article
- Structure and Reactivity of Glycosyl Isocyanides.European journal of organic chemistry · 2019Article
- Design of indole- and MCR-based macrocycles as p53-MDM2 antagonists.Beilstein journal of organic chemistry · 2019Article
- Artificial Macrocycles.Synlett : accounts and rapid communications in synthetic organic chemistry · 2018Article
- Concise Synthesis of Macrocycles by Multicomponent Reactions.Synthesis · 2018Article
- Synthetic fermentation of β-peptide macrocycles by thiadiazole-forming ring-closing reactions.Chemical science · 2018Article
- Two-Step Macrocycle Synthesis by Classical Ugi Reaction.The Journal of organic chemistry · 2018Article
- Ugi Multicomponent Reaction Based Synthesis of Medium-Sized Rings.Organic letters · 2017Article
- Concise Synthesis of Tetrazole Macrocycle.Organic letters · 2017Article
- Artificial Macrocycles by Ugi Reaction and Passerini Ring Closure.The Journal of organic chemistry · 2016Article
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
The design and synthesis of head-to-tail linked artificial macrocycles using the Ugi-reaction has been developed. This synthetic approach of just two steps is unprecedented, short, efficient and works over a wide range of medium (8-11) and macrocyclic (≥12) loop sizes. The substrate scope and functional group tolerance is exceptional. Using this approach, we have synthesized 39 novel macrocycles by two or even one single synthetic operation. The properties of our macrocycles are discussed with respect to their potential to bind to biological targets that are not druggable by conventional, drug-like compounds. As an application of these artificial macrocycles we highlight potent p53-MDM2 antagonism.
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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.