ArticleJournal of medicinal chemistry2014
Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 45 citations in OpenAlex.
- An Alkaloid Biosynthetic Gene Bundle in Animals.Journal of the American Chemical Society · 2026Article
- Exploring Marine Alkaloids: A Natural Approach to Cancer Treatment.Current pharmaceutical biotechnology · 2025Review
- The Interplay Between theInternational journal of molecular sciences · 2024Review
- Discovery of Anti-Inflammatory Alkaloids from SpongeMarine drugs · 2024Article
- TheMolecules (Basel, Switzerland) · 2023Article
- Synthesis of Agelastatin A and Derivatives Premised on a Hidden Symmetry Element Leading to Analogs Displaying Anticancer Activity.Tetrahedron · 2021Article
- Reaction of Papaverine with Baran DiversinatesMolecules (Basel, Switzerland) · 2019Article
- Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia.MedChemComm · 2019Article
- Synthesis and Evaluation of Agelastatin Derivatives as Potent Modulators for Cancer Invasion and Metastasis.The Journal of organic chemistry · 2017Article
- Inhibition of Eukaryotic Translation by the Antitumor Natural Product Agelastatin A.Cell chemical biology · 2017Article
- Cytotoxic Compounds Derived from Marine Sponges. A Review (2010-2012).Molecules (Basel, Switzerland) · 2017Review
- Radicals: Reactive Intermediates with Translational Potential.Journal of the American Chemical Society · 2016Review
- Derivatization of agelastatin A leading to bioactive analogs and a trifunctional probe.Bioorganic & medicinal chemistry letters · 2016Article
- Marine Natural Products from New Caledonia--A Review.Marine drugs · 2016Review
- Radical C-H functionalization of heteroarenes under electrochemical control.Angewandte Chemie (International ed. in English) · 2014Article
- Simple sulfinate synthesis enables C-H trifluoromethylcyclopropanation.Angewandte Chemie (International ed. in English) · 2014Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Chronic lymphocytic leukemia (CLL) is the most common lymphoid neoplasia in Western societies and is currently incurable. Multiple treatment options are practiced, but the available small molecule drugs suffer from dose-limiting toxicity and undesirable side effects. The need for new, less toxic treatments is a pressing concern. Here, we demonstrate that (-)-agelastatin A (1a), a pyrrole-imidazole alkaloid obtained from a marine sponge, exhibits potent in vitro activity against primary cell lines of CLL and disclose the synthesis of several analogues that are equipotent or exceed the potency of the natural product. The novel synthetic analogue, 13-debromo-13-trifluoromethyl agelastatin A (1j), showed higher activity than the natural product when tested against the same cell lines and is the most potent agelastatin derivative reported to date. A detailed in vitro structure-activity relationship of 1a in CLL compared to that of 22 synthetic analogues is described along with preliminary in vivo pharmacokinetic and metabolism studies on the most potent compounds.
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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.