Boron-Based Functionalities Enhance, the Potency of 2,5-Dimethylfuran-Based IDO1 Inhibitors.

Thomas J C Carraro, Samrat Dasgupta, Jacqueline Ku, Shane R Thomas, Louis M Rendina

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Article in Chembiochem : a European journal of chemical biology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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5 · Who and what money

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5 authors.

Thomas J C CarraroSchool of Chemistry, The University of Sydney, Sydney, NSW, 2006, Australia.

Samrat DasguptaSchool of Chemistry, The University of Sydney, Sydney, NSW, 2006, Australia.

Jacqueline KuSchool of Biomedical Sciences, Faculty of Medicine & Health, The University of New South Wales, Sydney, 2052, Australia.

Shane R ThomasSchool of Biomedical Sciences, Faculty of Medicine & Health, The University of New South Wales, Sydney, 2052, Australia.

Louis M RendinaSchool of Chemistry, The University of Sydney, Sydney, NSW, 2006, Australia.ORCID https://orcid.org/0000-0001-6539-6817

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Indoleamine-2,3-dioxygenase-1 (IDO1) is a critical immunoregulatory enzyme responsible for the metabolism of tryptophan during inflammation and disease. Based on a 2,5-dimethylfuran framework, examples of indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors containing a diverse set of boron-based functional groups (closo-1,2- and 1,7-carborane, boronic acids and esters, and benzoxaboroles) are reported. The novel boron derivatives display low micrometer affinity for the human recombinant enzyme, with IC50 values ranging from 8 to 60 μM. Superior results are observed for the closo-carborane compounds which demonstrate a significant improvement in potency over their phenyl analogues, with inhibition of the IDO1 enzyme increasing by up to ≈80%.

Indexed as

BoronBoron CompoundsEnzyme InhibitorsFuransIndoleamine-Pyrrole 2,3,-DioxygenaseHumansMolecular StructureStructure-Activity RelationshipBoronBoron CompoundsEnzyme InhibitorsFuransIDO1 protein, humanIndoleamine-Pyrrole 2,3,-Dioxygenaseboroncarboranesdrug discoveriesindoleamine‐2,3‐dioxygenase‐1inhibitors

Identifiers

PMID40183334

DOI10.1002/cbic.202500134

PMCPMC12177699

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LicenceCC BY-NC-ND

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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.