ArticleJournal of medicinal chemistry2014
Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity.
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 22 papers.
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Who cites it
22 citing papers in PubMed.
- Design, synthesis and antiviral activity of ciclopirox (CPX) analogs against orthopoxvirus.Bioorganic & medicinal chemistry · 2026Article
- 2-Pyridone-assisted palladium-catalyzed regioselective arylation of naphthamides.RSC advances · 2026Article
- The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer.Acta pharmaceutica Sinica. B · 2023Review
- Synthetic derivatives of the antifungal drug ciclopirox are active against herpes simplex virus 2.European journal of medicinal chemistry · 2022Article
- Glioblastoma: Current Status, Emerging Targets, and Recent Advances.Journal of medicinal chemistry · 2022Review
- Recent advances of IDH1 mutant inhibitor in cancer therapy.Frontiers in pharmacology · 2022Review
- Recent Advances of Pyridinone in Medicinal Chemistry.Frontiers in chemistry · 2022Review
- Synthetic Derivatives of Ciclopirox are Effective Inhibitors ofACS omega · 2021Article
- Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors.ACS medicinal chemistry letters · 2018Article
- Article
- Beyond Brooding on Oncometabolic Havoc in IDH-Mutant Gliomas and AML: Current and Future Therapeutic Strategies.Cancers · 2018Review
- Inhibition of Mutated Isocitrate Dehydrogenase 1 in Cancer.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2018Article
- Inhibition of Glycolysis and Glutaminolysis: An Emerging Drug Discovery Approach to Combat Cancer.Current topics in medicinal chemistry · 2018Review
- Allosteric inhibitor remotely modulates the conformation of the orthestric pockets in mutant IDH2/R140Q.Scientific reports · 2017Article
- Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.ACS medicinal chemistry letters · 2017Article
- Structure based discovery of clomifene as a potent inhibitor of cancer-associated mutant IDH1.Oncotarget · 2017Article
- Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.ACS medicinal chemistry letters · 2017Article
- 2-Hydroxypyridine-ACS medicinal chemistry letters · 2017Article
- Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives.Journal of hematology & oncology · 2016Review
- 3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1.Journal of medicinal chemistry · 2016Article
Corrections and comments
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Authors and funding
11 authors.
Funding
Abstract
Mutations of isocitrate dehydrogenase 1 (IDH1) are frequently found in certain cancers such as glioma. Different from the wild-type (WT) IDH1, the mutant enzymes catalyze the reduction of α-ketoglutaric acid to d-2-hydroxyglutaric acid (D2HG), leading to cancer initiation. Several 1-hydroxypyridin-2-one compounds were identified to be inhibitors of IDH1(R132H). A total of 61 derivatives were synthesized, and their structure-activity relationships were investigated. Potent IDH1(R132H) inhibitors were identified with Ki values as low as 140 nM, while they possess weak or no activity against WT IDH1. Activities of selected compounds against IDH1(R132C) were found to be correlated with their inhibitory activities against IDH1(R132H), as well as cellular production of D2HG, with R(2) of 0.83 and 0.73, respectively. Several inhibitors were found to be permeable through the blood-brain barrier in a cell-based model assay and exhibit potent and selective activity (EC50 = 0.26-1.8 μM) against glioma cells with the IDH1 R132H mutation.
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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.