ArticleJournal of medicinal chemistry2008
Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors.
Article in Journal of medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 38 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
38 citing papers in PubMed, 165 citations in OpenAlex.
- Catalyst-Controlled Divergent Annulation Reactions of Allenoates and Fully Substituted 1,3-Indandione Derived Electron-Deficient Alkenes.The Journal of organic chemistry · 2026Article
- Dual-action mitochondria-targeted prodrugs that both deplete mitochondrial glutathione and deliver a toxic payload to the matrix.European journal of medicinal chemistry · 2026Article
- Artemether and Euphorbia factor L9 suppress kynurenine production through distinct effects on tryptophan metabolism.The Biochemical journal · 2026Article
- Naphthoquinone-derived tridentate Ru(II) and Os(II) organometallics with exceptional cytotoxicity: synthesis, characterization, stability in aqueous solution and biologicalDalton transactions (Cambridge, England : 2003) · 2026Article
- Molecular Hybridization of Naphthoquinones and Thiazoles: A Promising Strategy for Anticancer Drug Discovery.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Substituted 1,4-naphthoquinones for potential anticancer therapeutics:Computational and structural biotechnology journal · 2025Article
- Molecular Docking and Dynamics Simulation Studies Predict Potential Anti-ADAR2 Inhibitors: Implications for the Treatment of Cancer, Neurological, Immunological and Infectious Diseases.International journal of molecular sciences · 2023Article
- Benzochromenopyrimidines: Synthesis, Antiproliferative Activity against Colorectal Cancer and Physicochemical Properties.Molecules (Basel, Switzerland) · 2022Article
- Synthesis and investigation of antiproliferative activity of Ru-NHC complexes against C6 and HeLa cancer cells.Turkish journal of chemistry · 2022Article
- Indoleamine 2, 3-dioxygenase 1 inhibitory compounds from natural sources.Frontiers in pharmacology · 2022Review
- Menadione: a platform and a target to valuable compounds synthesis.Beilstein journal of organic chemistry · 2022Review
- Biologically active marine natural products and their molecular targets discovered using a chemical genetics approach.Natural product reports · 2020Review
- Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.MedChemComm · 2019Review
- Inflammatory Reprogramming with IDO1 Inhibitors: Turning Immunologically Unresponsive 'Cold' Tumors 'Hot'.Trends in cancer · 2018Review
- Indoleamine 2,3-Dioxygenase and Its Therapeutic Inhibition in Cancer.International review of cell and molecular biology · 2018Review
- Discovery of IDO1 Inhibitors: From Bench to Bedside.Cancer research · 2017Review
- Trial Watch-Small molecules targeting the immunological tumor microenvironment for cancer therapy.Oncoimmunology · 2016Review
- O-alkylhydroxylamines as rationally-designed mechanism-based inhibitors of indoleamine 2,3-dioxygenase-1.European journal of medicinal chemistry · 2016Article
- Respiratory Syncytial Virus-Infected Mesenchymal Stem Cells Regulate Immunity via Interferon Beta and Indoleamine-2,3-Dioxygenase.PloS one · 2016Article
- Targeting the indoleamine 2,3-dioxygenase pathway in cancer.Journal for immunotherapy of cancer · 2015Review
Corrections and comments
- Erratum issued
Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
Indoleamine 2,3-dioxygenase (IDO) is emerging as an important new therapeutic target for the treatment of cancer, chronic viral infections, and other diseases characterized by pathological immune suppression. While small molecule inhibitors of IDO exist, there remains a dearth of high-potency compounds offering in vivo efficacy and clinical translational potential. In this study, we address this gap by defining a new class of naphthoquinone-based IDO inhibitors exemplified by the natural product menadione, which is shown in mouse tumor models to have similar antitumor activity to previously characterized IDO inhibitors. Genetic validation that IDO is the critical in vivo target is demonstrated using IDO-null mice. Elaboration of menadione to a pyranonaphthoquinone has yielded low nanomolar potency inhibitors, including new compounds which are the most potent reported to date (K(i) = 61-70 nM). Synthetic accessibility of this class will facilitate preclinical chemical-genetic studies as well as further optimization of pharmacological parameters for clinical translation.
Indexed as
Identifiers
What OpenQuestion holds
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.