ArticleScientific reports2019
A landmark in drug discovery based on complex natural product synthesis.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- First-In-Human Study: Dose Expansion of E7130 in Urothelial Carcinoma and Squamous Cell Carcinoma of the Head and Neck.Cancer science · 2026Article
- Fibroblasts as Turned Agents in Cancer Progression.Cancers · 2023Review
- Natural products and drug discovery.National science review · 2022Review
- A unified strategy for the total syntheses of eribulin and a macrolactam analogue of halichondrin B.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Old and modern antibiotic structures with potential for today's infections.ADMET & DMPK · 2022Review
- Self-assembly of an anion receptor with metal-dependent kinase inhibition and potent in vitro anti-cancer properties.Nature communications · 2021Article
- The quest for supernatural products: the impact of total synthesis in complex natural products medicinal chemistry.Natural product reports · 2020Review
- Bioactive compounds from marine invertebrates as potent anticancer drugs: the possible pharmacophores modulating cell death pathways.Molecular biology reports · 2020Review
Corrections and comments
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Authors and funding
21 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Despite their outstanding antitumour activity in mice, the limited supply from the natural sources has prevented drug discovery/development based on intact halichondrins. We achieved a total synthesis of C52-halichondrin-B amine (E7130) on a >10 g scale with >99.8% purity under GMP conditions. Interestingly, E7130 not only is a novel microtubule dynamics inhibitor but can also increase intratumoural CD31-positive endothelial cells and reduce α-SMA-positive cancer-associated fibroblasts at pharmacologically relevant compound concentrations. According to these unique effects, E7130 significantly augment the effect of antitumour treatments in mouse models and is currently in a clinical trial. Overall, our work demonstrates that a total synthesis can address the issue of limited material supply in drug discovery/development even for the cases of complex natural products.
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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.