ArticleMolecular pharmacology2012
Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.
Article in Molecular pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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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
34 citing papers in PubMed, 87 citations in OpenAlex.
- Chemistry and Biological Activity of 11Molecules (Basel, Switzerland) · 2026Review
- Synthesis of novel 11H-indeno[1,2-b]quinoxaline derivatives and their in vitro and in silico insights into anticancer activities.Scientific reports · 2026Article
- 6-(2-Aminoethyl)-6Biomolecules · 2026Article
- Crystal structure of (Acta crystallographica. Section E, Crystallographic communications · 2026Article
- Crystal structures of the homologues diethyl and dimethyl (10Acta crystallographica. Section E, Crystallographic communications · 2026Article
- c-Jun N-Terminal Kinase (JNK) Inhibitor IQ-1S as a Suppressor of Tumor Spheroid Growth.Molecules (Basel, Switzerland) · 2025Article
- Heterogeneity and interplay: the multifaceted role of cancer-associated fibroblasts in the tumor and therapeutic strategies.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2024Review
- Evaluation of Nitric Oxide-Donating Properties of 11Molecules (Basel, Switzerland) · 2024Article
- Anti-Inflammatory Activity of Pyrazolo[1,5-Molecules (Basel, Switzerland) · 2024Article
- Effect of IQ-1 on the Infarct Size and the Parameters of Cardiodynamic Indicators in the Acute Period after Myocardial Ischemia/Reperfusion in Rats.Bulletin of experimental biology and medicine · 2024Article
- Development and Assessment of 1,5-Diarylpyrazole/Oxime Hybrids Targeting EGFR and JNK-2 as Antiproliferative Agents: A Comprehensive Study through Synthesis, Molecular Docking, and Evaluation.Molecules (Basel, Switzerland) · 2023Article
- Neuroprotective Effects of Tryptanthrin-6-Oxime in a Rat Model of Transient Focal Cerebral Ischemia.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Experimental and Computational Investigation of the Oxime Bond Stereochemistry in c-Jun N-terminal Kinase 3 Inhibitors 11Pharmaceutics · 2023Article
- Novel Tryptanthrin Derivatives with Selectivity asMolecules (Basel, Switzerland) · 2023Article
- Cardioprotective Effects of a Selective c-Jun N-terminal Kinase Inhibitor in a Rat Model of Myocardial Infarction.Biomedicines · 2023Article
- Suppression of Age-Related Macular Degeneration-like Pathology by c-Jun N-Terminal Kinase Inhibitor IQ-1S.Biomedicines · 2023Article
- Neuroprotective Effects of the Lithium Salt of a Novel JNK Inhibitor in an Animal Model of Cerebral Ischemia-Reperfusion.Biomedicines · 2022Article
- Pyridazinones and Structurally Related Derivatives with Anti-Inflammatory Activity.Molecules (Basel, Switzerland) · 2022Article
- Green Synthesis of Indeno[1,2-b]quinoxalines Using β-Cyclodextrin as Catalyst.Molecules (Basel, Switzerland) · 2022Article
- Design, synthesis and biological evaluation of novel O-substituted tryptanthrin oxime derivatives as c-JunFrontiers in pharmacology · 2022Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
In efforts to identify novel small molecules with anti-inflammatory properties, we discovered a unique series of tetracyclic indenoquinoxaline derivatives that inhibited lipopolysaccharide (LPS)-induced nuclear factor-κB/activating protein 1 activation. Compound IQ-1 (11H-indeno[1,2-b]quinoxalin-11-one oxime) was found to be a potent, noncytotoxic inhibitor of pro-inflammatory cytokine [interleukin (IL)-1α, IL-1β, IL-6, IL-10, tumor necrosis factor (TNF)-α, interferon-γ, and granulocyte-macrophage colony-stimulating factor] and nitric oxide production by human and murine monocyte/macrophages. Three additional potent inhibitors of cytokine production were identified through further screening of IQ-1 analogs. The sodium salt of IQ-1 inhibited LPS-induced TNF-α and IL-6 production in MonoMac-6 cells with IC(50) values of 0.25 and 0.61 μM, respectively. Screening of 131 protein kinases revealed that derivative IQ-3 [11H-indeno[1,2-b]quinoxalin-11-one-O-(2-furoyl)oxime]was a specific inhibitor of the c-Jun N-terminal kinase (JNK) family, with preference for JNK3. This compound, as well as IQ-1 and three additional oxime indenoquinoxalines, were found to be high-affinity JNK inhibitors with nanomolar binding affinity and ability to inhibit c-Jun phosphorylation. Furthermore, docking studies showed that hydrogen bonding interactions of the active indenoquinoxalines with Asn152, Gln155, and Met149 of JNK3 played an important role in enzyme binding activity. Finally, we showed that the sodium salt of IQ-1 had favorable pharmacokinetics and inhibited the ovalbumin-induced CD4(+) T-cell immune response in a murine delayed-type hypersensitivity model in vivo. We conclude that compounds with an indenoquinoxaline nucleus can serve as specific small-molecule modulators for mechanistic studies of JNKs as well as a potential leads for the development of anti-inflammatory drugs.
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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.