ArticleNature chemistry2018
Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3.
Article in Nature chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
44 citing papers in PubMed, 116 citations in OpenAlex.
- A pro-natural product design strategy affords ester-based green fungicide candidates.Science advances · 2026Article
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- Pseudonatural Products for Chemical Biology and Drug Discovery.Journal of medicinal chemistry · 2025Review
- Photochemically-Enabled Umpolung Conversion of 2-Acyloxybenzaldehydes into 2-Hydroxybenzofuranones.Molecules (Basel, Switzerland) · 2025Article
- Progress of research on glucose transporter proteins in hepatocellular carcinoma.World journal of hepatology · 2025Review
- The Role of Glycolipids and their Toxicity in the Context of Nanomaterials and Nanoparticles: A Review of the Literature.Current drug targets · 2025Review
- Research Progress and Prospect of Nitrogen-containing Heterocycle in Anti-gastric Cancer Drugs: A Review.Current medicinal chemistry · 2025Review
- Article
- Pan-cancer analysis of SLC2A family genes as prognostic biomarkers and therapeutic targets.Heliyon · 2024Article
- Targeting the Warburg effect: A revisited perspective from molecular mechanisms to traditional and innovative therapeutic strategies in cancer.Acta pharmaceutica Sinica. B · 2024Review
- Role of long non-coding RNAs in metabolic reprogramming of gastrointestinal cancer cells.Cancer cell international · 2024Review
- Functional importance of glucose transporters and chromatin epigenetic factors in Glioblastoma Multiforme (GBM): possible therapeutics.Metabolic brain disease · 2023Review
- Information-Rich, Dual-FunctionJournal of the American Chemical Society · 2023Article
- The Time and Place for Nature in Drug Discovery.JACS Au · 2022Review
- Identification of a Novel Pseudo-Natural Product Type IV IDO1 Inhibitor Chemotype.Angewandte Chemie (International ed. in English) · 2022Article
- Targeting Glucose Metabolism Enzymes in Cancer Treatment: Current and Emerging Strategies.Cancers · 2022Review
- The Pseudo-Natural Product Rhonin Targets RHOGDI.Angewandte Chemie (International ed. in English) · 2022Article
- Chemical Evolution of Natural Product Structure.Journal of the American Chemical Society · 2022Article
- Natural product drug discovery in the artificial intelligence era.Chemical science · 2022Review
- Pseudonatural Products Occur Frequently in Biologically Relevant Compounds.Journal of chemical information and modeling · 2021Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The principles guiding the design and synthesis of bioactive compounds based on natural product (NP) structure, such as biology-oriented synthesis (BIOS), are limited by their partial coverage of the NP-like chemical space of existing NPs and retainment of bioactivity in the corresponding compound collections. Here we propose and validate a concept to overcome these limitations by de novo combination of NP-derived fragments to structurally unprecedented 'pseudo natural products'. Pseudo NPs inherit characteristic elements of NP structure yet enable the efficient exploration of areas of chemical space not covered by NP-derived chemotypes, and may possess novel bioactivities. We provide a proof of principle by designing, synthesizing and investigating the biological properties of chromopynone pseudo NPs that combine biosynthetically unrelated chromane- and tetrahydropyrimidinone NP fragments. We show that chromopynones define a glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and -3, inhibits cancer cell growth and promises to inspire new drug discovery programmes aimed at tumour metabolism.
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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.