ArticleMolecular diversity2025
Design, synthesis, and biological evaluation of novel molecules as potent inhibitors of indoleamine 2,3-dioxygenase 1.
Article in Molecular diversity, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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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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Who cites it
1 citing paper in PubMed.
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Authors and funding
9 authors.
Funding
Abstract
Tumoral immune escape is an obstacle to successful cancer therapy. Tryptophan catabolism mediated by indoleamine 2,3-dioxygenase (IDO1) is an important mechanism of peripheral immune tolerance contributing to tumoral immune resistance, and IDO1 inhibition is an active area of drug development. Several classes of small molecule-based IDO1 inhibitors have already been reported. Still, only a few compounds are currently being evaluated in various stages of clinical trials as adjuvants or in combination with chemo- and radiotherapies. In this study, a novel series of 1,2,5-oxadiazole-3-carboximidamide derivatives were designed, synthesized, and evaluated for inhibitory activities against IDO1, and their structure-activity relationship was investigated. Notably, several compounds (11c, 11j, 11o, and 11u) showed powerful anti-tumor effects in the low micromolar range. Among them, compound 11u exhibited excellent inhibitory potency against hIDO1 (IC
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