ArticleACS medicinal chemistry letters2025
Design, Synthesis, and Biological Evaluation of Dual Functional Inhibitors Targeting Indoleamine 2,3-dioxygenase 1 (IDO1) and Tryptophan 2,3-dioxygenase (TDO).
Article in ACS medicinal chemistry letters, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers, 1 of them a synthesis that pooled it.
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.
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.
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Who cites it
4 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Epstein-Barr virus-driven immunosuppression in nasopharyngeal carcinoma: a comprehensive review of viral mechanisms, spatial tumor ecosystems, and precision therapeutics.Frontiers in immunology · 2026Pooled it
- Janus Reactivity of a Mononuclear Non-Heme Iron(III)-Peroxo Complex Toward Indole Oxidation.Angewandte Chemie (International ed. in English) · 2026Article
- Discovery of a Dual IDO1/TDO Inhibitor That Modulates Enzymatic Activity and IDO1/SHP-2 Signaling.Journal of medicinal chemistry · 2026Article
- Design, Synthesis, and Biological Evaluation of Novel Morpholine-Coumarin Derivatives for Inflammation-Associated Depression.Biomolecules · 2026Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
Tryptophan metabolism via the kynurenine pathway plays a critical role in immune regulation and neurobiology. Dysregulation of this pathway, particularly through overactivation of indoleamine 2,3-dioxygenases (IDOs) and tryptophan 2,3-dioxygenase (TDO), has been implicated in various pathological conditions, including cancer, depression, chronic pain, and neurodegenerative diseases. Here, we report the design and synthesis of a novel class of dual IDO1/TDO inhibitors featuring a 5,6-dihydroimidazothiazole core linked to a urea motif via an alkyl spacer. These compounds were evaluated for their inhibitory activity against IDO1 and TDO using cellular-based enzymatic activity assays. Most compounds demonstrated higher potency toward IDO1, as indicated by EC
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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.